POLAR-SUBSTITUTED HYDROCARBONS

Abstract: The invention relates to retroviral protease inhibitors of the general formula (I): W-(A)n-B-(A*)m-V where W, A, B, A*, V, n and m are as defined herein, including related prodrugs of general formula (I) comprising a solubilising group which is labile in vivo.

Description: POLAR-SUBSTITUTED HYDROCARBONS TECHNICAL FIELD The invention relates to certain hydrocarbon derivatives bearing polar substituents and their use in the inhibition of retroviral proteases, for example in the 5 treatment of HIV viral infections such as acquired immunodeficiency syndrome (AIDS). The invention also relates to processes for preparing such hydrocarbon derivatives bearing polar substituents, to pharmaceutical compositions comprising them and to methods for the treatment or prophylaxis of retroviral infections. The invention also relates to a process for enhancing the water-solubility of a pharmaceutical or veterinary substance. io BACKGROUND ART Human immunodeficiency virus (HIV) is a pathogenic retrovirus causing AIDS and its related disorders. The development of antiviral chemotherapy against AIDS has been the subject of an intense research effort since the discovery of HIV. (For a recent review on molecular targets for AIDS therapy see Mitsua et al, Science, 1990, pp 1533- 15 1544). The HIV Proteases (HIV PR), and aspartyl proteases, were first suggested as a potential target for AIDS therapy by Kramer et al. (Science 231, 1580 (1986)). Since that time the potential usefulness of HIV PR inhibitors as effective agents in treatment of AIDS has been widely recognized (for a review of the HIV PR as a therapeutic target see Tomaselli et al. Chimica Oggi, May 1991, pp 6-27 and Huff J.R., J. Med. Chem. 34, 20 2314-2327 (1991)). Of the classical transition state mimics for aspartyl proteases, the hydroxy ethylene, dihydroxy ethylene, hydroxyethylamine and phosphinic acid isosteres appear to provide the greatest affinity for HIV PR. Many inhibitors of HIV PR have been shown to have an antiviral activity at concentrations in the nanomolar range in the different cell systems and are described as such in the patent literature. 25 OBJECTS OF THE INVENTION It is an object of the present invention to provide compounds useful as retroviral protease inhibitors. It is another object of the present invention to provide pharmaceutical compositions comprising compounds useful for the treatment or prophylaxis of retroviral infections. It is a further object of the present invention to provide methods for the 30 treatment or prophylaxis of retroviral infections, in particular AIDS. Other objects of the present invention are to provide processes for preparing compounds useful as retroviral protease inhibitors, and processes for enhancing the water-solubility of pharmaceutical or veterinary substances, in particular retroviral protease inhibitors. SUMMARY OF THE INVENTION 35 The invention provides compounds which are useful as inhibitors of retroviral proteases, particularly aspartyl proteases and more particularly HIV proteases, and which are effective in treating conditions characterized by unwanted activity of these enzymes, in particular acquired immune deficiency syndrome. In the following description of the invention, the teaching of each of the publications mentioned is incorporated herein by reference. A first embodiment of the invention is directed to compounds of the general formula (I) or pharmaceutically acceptable salts or prodrugs thereof: W-(A) n -B-(A*) m -V 0 ) wherein W is selected from the group consisting of Rj-X-, R^-X*-, -Y*, -CN, -N=CR 5 R 5* , -C(R 5 )=NR 3 , -C(R 5 )=NOR 3 , -C(NR 3 R 4 )=NR 5 **, -C(D)OR 3 , -C(D)SR 3 and -C(D)NR 3 R 4 , wherein Y* is as defined below, R l s R 3 and R 4 are independently selected from the group consisting of Rg and a solubilising group Px which is labile in vivo, wherein Rg is selected from the group consisting of hydrogen, R 20 , wherein R 20 is selected from the group consisting of optiona l: ly substituted (C r C 18 )alkyl, optiona lly substituted (C 2 -Cι 8 )alkenyl, optiona lly substituted (C 2 -Cι )alkynyl, optiona lly substituted (C 3 -C 18 )cycloalkyl, optiona lly substituted (C 3 -C 18 )cycloalkyl(C r C 18 )alkyl, optiona l:ly substituted (C 3 -C 18 )cycloalkyl(C 2 -C 18 )alkenyl, optiona lly substituted (C 3 -C 18 )cycloalkyl(C 2 -Cι 8 )alkynyl, optiona lly substituted (C 6 -C 24 )aryl, optiona llly substituted (C 6 -C 24 )aryl(C r C 18 )alkyl, optiona lly substituted (C 6 -C 24 )aryl(C 2 -C 18 )alkenyl, optiona lly substituted (C 6 -C 24 )aryl(C 2 -C 18 )alkynyl, optiona lly substituted (C C 18 )acyl, optiona lly substituted heterocyclic, optiona lly substituted heterocyclic C j -C^alkyl, optiona lly substituted heterocyclic(C 2 -Cι 8 )alkenyl, and optiona l: ly substituted heterocyclic(C 2 -C 18 )alkynyl C(D)OR 21 , C(D)SR 21 , C(D)NR 21 R 22 , C(NR 21 )R 22 , C(NR 21 )OR 22 , and C(NR 21 )NR 22 R 23 , wherein R 21 , R 22 and R 3 independently are selected from hydrogen and R 20 as previously defined, or R 21 and R 22 together, or R 22 and R 23 together form a . saturated or unsaturated cyclic, bicyclic or fused ring system as defined below, or R 3 and R4, when present, together form a saturated or unsaturated cyclic, bicyclic or fused ring system as defined below, D is selected from O and S, X is selected from the group consisting of Y, S(O) and S(O) 2 wherein Y is as defined below, X* is selected from the group consisting of NR 10 , O and S, wherein R 10 has the meaning of R as previously defined, R j * is selected from the group consisting of R j as previously defined, P(O)(OR 7 )R 8 , S(O) z OR 7 and S(O) z NR 7 R 8 , wherein z is 1 or 2 and R 7 and R 8 independently have the meaning of R 20 as previously defined, or R 7 and R 8 together form a saturated or unsaturated cyclic, bicyclic or fused ring system as defined below, R 5 and R 5 * are independently selected from the group consisting of H, CF 3 , C(D)OR 103 , C(D)SR 103 C(D)NR 103 R 10 4 and R 20 as previously defined, wherein D is as previously defined, and wherein R 103 and R 104 have the meaning of R as previously defined, or R 103 and R 104 together form a saturated or unsaturated cyclic, bicyclic or fused ring system as defined below, and R 5 ** is selected from hydrogen and R 20 as previously defined; n is 0-6; m is 0-6 and n+m > 1; A at each occurrence is independently selected from the group consisting of and a residue of a naturally occurring or synthetic amino acid; A* at each occurrence is independently selected from the group consisting of and a residue of a naturally occurring or synthetic amino acid; wherein R 12 *, Rι 3 *, R9 and R 9 * are independently selected from the group consisting of F, Cl, Br, I and R5 as previously defined, Rn has the meaning of Rj as previously defined, R 12 has the meaning of Rg as previously defined, R 13 is selected from the group consisting of F, Cl, Br, I, Rg as previously defined, and R 20 o, wherein R 20 o is selected from the group consisting of CN, NCO, NCS, OCN, SCN, ORgo, SRgo> NRgoRθi, D 1 C(D 2 )R 60 , D 1 C(D 2 )D 3 R 60 , D 1 C(D 2 )NR 6 oRg 1 , NRg 0 C(D 1 )R 61 , NR 6 oC(D 1 )D 2 R 61 , NR 60 C(D 1 )NR 61 R6 2 , NRgoORg ! , amidino, guanidino, S(O)R6o, S(O)NR 60 R 61 , S^^NRgoRg j , D^^RgQ, D 1 S(O) 2 OR 60 , D 1 S(O) 2 NR 60 R 6 ι, P(D 1 )(D 2 R 6 o)R 6 ι, P(D 1 )(D 2 R 60 )D 3 R 61 , P(D 1 )(D 2 R 6 o)NR 61 R 62 , P(D 1 )R 60 R 6 ι, D 1 P(D 2 )(D 3 R 60 )R 61 , D 1 P(D 2 )(D 3 R 60 )D 4 R 61 , D 1 P(D 2 )(D 3 R 60 )NR 61 R 62 , D 1 P(D 2 )R 60 R6i, NR 60 NR 61 R 62 and wherein D l s D 2 , D 3 and D 4 independently have the meaning of D as previously defined, and R_ 60 , and Rg 2 independently have the meaning of Rg as previously defined or any two or more of R Q , R^ and Rg 2 form part of a saturated or unsaturated cyclic, bicyclic or fused ring system as defined below, or R 12 and Rχ 3 together are selected from the group consisting of =O, =S, / Reo = C . 1 =NOR 60 , =NR 60 , -OQO-, -SQS- and -SQO-, wherein Q is optionally substituted (Cι-C 12 )alkylidene as defined below and R^ Q is as previously defined, and L is selected from the group consisting of a bond, D D II II — C— N— — N-C— I I R11 R11 — O— — S— — S(0)z— ) ) ) ) s — N — — S(0) z -N — — N— S(0) z - — N— S(0) z N — Rn R11 R11 R11 Rn* » -CH 2 - and -CH 2 -CH 2 -, wherein R π and D are as previously defined, R * and D* have the meaning of R n and D respectively, and z is 1 or 2; R 13 ** is F, Cl, Br, OR^o or NR^Rgo wherein Rgo and R^γ are as previously defined, B is selected from the group consisting of - — — — — — - — — p — — — — — Rl4* R-I4 R14 D * D* o o OR18 OR15 -C— — C— I and I SR-|9 NR-|8*Rl9* wherein R 203 and R 2 03* independently have the meaning of R $ as previously defined, Rl4* and R^** are independently selected from the group consisting of hydrogen, R 2 n . as previously defined, CF 3 , C(D*)OR4 0 , C(D*)SR4o and C(D*)NR 40 R 4 ι, wherein R40 and R 1 independently have the meaning of R 2 ι and R 22 as previously defined or R40 and R41 form part of a saturated or unsaturated cyclic, bicyclic or fused ring system as defined below, R14 is selected from the group consisting of F, Cl, Br, I, R 14 * as previously defined and R 2 QO as previously defined, R17 and R 17 * independently have the meaning of Rg as previously defined, D* has the meaning of D as previously defined, Z is a samrated or unsaturated (C 2 -C4)alkylidene radical which is optionally substituted with one or more groups selected from F, Cl, Br, I and R 1 * as previously defined, Z* is a saturated or unsamrated (C 1 -C 3 )alkylidene radical which is optionally substituted with one or more groups selected from F, Cl, Br, I and R 1 * as previously defined, M j is selected from the group consisting of OR 15 , SR 15 and NR 15 R 17 , wherein R^ is selected from the group consisting of: Px as previously defined, and R as previously defined, and a glycosyl radical which is derived from a synthetic or naturally occurring aldose, ketose, deoxyaldose, deoxyketose, aminoaldose, aminoketose or an oligosaccharide thereof, and R17 is as previously defined, or R 15 and R 17 together form a saturated or unsamrated cyclic, bicyclic or fused ring system as defined below, M and M* are independently selected from the group consisting of M j as previously defined, OCN, SCN, YR 2 , Y* and N=CR 30 R 31 , wherein Y, Y* and R 2 are as defined below, and R 30 and R 31 independently have the meaning of R 20 as previously defined, M 2 is selected from the group consisting of R 1 * as previously defined, -CR 30 *=Y** and -CR 30 *=NR 17 *, where Y** is as defined below, R 30 * has the meaning of R 2 o as previously defined, and R J7* is as previously defined, R 18 and R 19 independently have the meaning of R 20 as previously defined or R 18 and R 19 together form part of a saturated or unsaturated cyclic, bicyclic or fused ring system as defined below, and R 18 * and R j9 * together form part of a saturated or unsaturated cyclic, bicyclic or fused ring system as defined below; V is selected from the group consisting of YR 2 , Y* and C(R 30 )=Y**, wherein Y is absent or is selected from the group consisting of: o o- o- II I — S— N — — N=N— — N=N — — N=N— + + ^50 O O o II II II -S-N— -N-S — — N— S — II I I II -o-s II- O R 50 RδC R50O o o o o o II II II II -s-o— — s— s — -o— s— — s-o — II II o o o O O n H ll — S— S — — S— S — — P— N — — O— P— N — O R51O R50 R51C R50 0 0 0 o ii ii ii ii — N— P— — N— P-O— — P-O- — O— P — I I I I I R 50 OR 51 R50OR51 OR 51 0R 51 > > > > o 0 0 o II II II II — P— N — — N— P — — P— O— — O— P — I I I I I I and R51O R50 R50OR51 D ** R 52 D ** R 52 wherein D** is selected from the group consisting of a bond, O, S and NR 50 , R 50 has the meaning of R as previously defined, R 51 has the meaning of R 15 as previously defined and R 52 has the meaning of R 20 as previously defined, or R 50 and R 51 , when present, together form part of a saturated or unsaturated cyclic, bicyclic or fused ring system as defined below, and R 2 has the meaning of R as previously defined, Y* is selected from the group consisting of R33 — N— N-R 2 * — N— N=C — N-O-R2* — O— N-R 2 * 1 1 ^ I R I I R50 R51 R50 "^ R50 R50 o O II II — s=o — s=o D ** R 115 -S=NRn7* I I -P=D* ■ N=0 R114* R 114* R114* I and R114** R114* — P=D * I wherein D* and D** independently have the meaning of D as R 114* * previously defined; Rn4*, Rπ4**, R115 and R 11 7* have the meaning of R14*, R14**, Rχ5 and R 17 * respectively, as previously defined; R 50 and R51 are as previously defined or R 50 and R 51 together form part of a saturated or unsaturated cyclic, bicyclic or fused ring system as defined below; R 2 * is selected from the group consisting of R 2 as previously defined, Px as previously defined, S(O) Z ORI 2 Q and S(O) z NR 120 Rι 2 ι, wherein z is 1 or 2; R 33 and R 3 4 are independently selected from the group consisting of hydrogen and R 2 o as previously defined, or R 33 and R 34 together form a saturated or unsaturated cyclic, bicyclic or fused ring system as defined below, and R 12 Q and R 12 j independently have the meaning of R Q as previously defined, or R 12 o and R 121 together form a saturated or unsamrated cyclic, bicyclic or fused ring system as defined below, R 30 is as previously defined, and Y** is selected from =N-NR 115 R 117 and =N-OR 115 , wherein R 115 and R 117 have the meaning of R 15 and Rg respectively, as previously defined, or R 115 and Rn7 together form a saturated or unsaturated cyclic, bicyclic or fused ring system as defined below, and wherein any group selected from Rγ, R 1Ψ , R 2 , R 2 *, R9, Rn > R i2 > R 13> R 14, R i4*> R 17 , R 50 and R 51 may, together with any other group selected from R l 5 R j *, R 2 , R 2 *, R 9 *, Rιo> Rn> R-12' R-13' R-14, R-i4*> R-i7» R50 and R51 form one or more saturated or unsamrated cyclic, bicyclic or fused ring system(s) as defined below, -^N-0 and wherein any tertiary amino nitrogen atom may be replaced by the group and, wherein any hydroxyl, mercapto or amino group may be protected by a protecting group which is labile in vivo. Compounds of the general formula (I) are useful as inhibitors of retroviral proteases, in particular HIV proteases. One form of the first embodiment of the invention is directed to compounds of the general formula (I') or pharmaceutically acceptable salts or prodrugs thereof: W-CA' -B'-CA' + -V i wherein W is selected from the group consisting of Ri-X-, R^-X*-, -Y*, -CN, -N=CR 5 R 5* , -C(R 5 )=NR 3 , -C(R 5 )=NOR 3 , -C(D)OR 3 , -C(D)SR 3 and -C(D)NR 3 R 4 , wherein Y* is as defined below, R l , R 3 and R 4 are independently selected from the group consisting of Rg and a solubilising group Px which is labile in vivo, wherein R^ is selected from the group consisting of hydrogen, R 20 , wherein R 2Q is selected from the group consisting of optiona. ly substituted (Cι-C 8 )alkyl, optiona ly substituted (C 2 -Cι 8 )alkenyl, optiona: ly substituted (C 2 -C 8 )alkynyl, optiona ly substituted (C 3 -Cι 8 )cycloalkyl, optiona: ly substituted (C 3 -C 18 )cycloalkyl(C r C 18 )alkyl, optiona ly substituted (C 3 -C 8 )cycloalkyl(C 2 -C 18 )alkenyl, optiona: ly substituted (C 3 -Cι 8 )cycloalkyl(C 2 -C 18 )alkynyl, optiona ly substituted (Cg-C^aryl, optiona: ly substituted (C 6 -C 24 )aryl(C r C 18 )alkyl, optiona ly substituted (C 6 -C 24 )aryl(C 2 -C 18 )alkenyl, optiona ly substituted (C 6 -C 24 )aryl(C 2 -C 18 )alkynyl, optiona ly substituted (C r C 8 )acyl, optiona: ly substituted heterocyclic, optiona ly substituted heterocyclic(C r C 18 )alkyl, optiona ly substituted heterocyclic(C 2 -C 18 )alkenyl, and optiona: ly substituted heterocyclic(C 2 -C 18 )alkynyl C(D)OR 21 , C(D)SR 21 , and C(D)NR 2 R 22 , wherein R 21 and R 22 independently are selected from hydrogen and R 0 as previously defined, or R 2 and R 22 together form a saturated or unsamrated cyclic, bicyclic or fused ring system as defined below, or R 3 and R4, when present, together form a saturated or unsamrated cyclic, bicyclic or fused ring system as defined below, D is selected from O and S, X is selected from the group consisting of Y', S(O) and S(O) 2 wherein Y 1 is as defined below, X* is selected from the group consisting of NR10, O and S, wherein R^ has the meaning of R^ as previously defined, Rl* is selected from the group consisting of Ri as previously defined, S(O) z OR 7 and S(O) z NR 7 R 8 , wherein z is 1 or 2 and R 7 and R 8 independently have the meaning of R 2 Q as previously defined, or R7 and R 8 together form a saturated or unsamrated cyclic, bicyclic or fused ring system as defined below, R 5 and R 5 * are independently selected from the group consisting of H, CF 3 , C(D)OR 103 , C(D)SRι 03 C(D)NRι 03 R 104 and R 20 as previously defined, wherein D is as previously defined, and wherein Rι 03 and R104 have the meaning of Rβ as previously defined, or Rι 03 and R104 together form a saturated or unsamrated cyclic, bicyclic or fused ring system as defined below; n' is 0-8; m' is 0-8 and n' +m' > 1; A' and A'* are independently at each occurrence selected from the group consisting of O, S, S(O), S(O) 2 , NR n , CR 12 R 13 and CR 12 *R !3 *, or two consecutive groups A' -A' or A'*-A'* are a structural unit selected from — C≡≡C — » wherein and Ri2* > Ri3* > R9 and R 9 * are independently selected from the group consisting of F, Cl, Br, I and R 5 as previously defined, Ru has the meaning of R as previosly defined, R 2 has the meaning of R as previously defined, R i3 is selected from the group consisting of F, Cl, Br, I, R as previously defined, and R 2 oo wherein R 2 oo is selected from the group consisting of CN, NCO, NCS, OCN, 5 SCN, N 3 , OR60> SR60» NRgoRβ!, io OiC jfRβo, O l Cφ 2 )O 3 R ω , DιC(D 2 )NR 60 R 6 ι, NR 60 C(D 1 )R 6 ι, NR 60 C(D 1 )D 2 R 61 , 15 NR 60 C(D 1 )NR 6 ιR 62 , NRfioORg!, amidino, guanidino, S(OJRβo, S^NRfioRg!, SCO NRβoRβi. DiS^R^, DιS(O) 2 OR6o, P(Dι)(D 2 R 60 )R 61 , P(D 1 )(D 2 R 6 o)D 3 R 61 , P(Dι)(D 2 R 60 )NR 6 ιR 62 , so P(Dι)R 60 R 6 ι, DιP(D 2 )(D 3 R 60 )R 61 , D 1 P(D 2 )(D 3 R 60 )D 4 R 61 , D 1 P(D 2 )(D 3 R 60 )NR 61 R 62 , D 1 P(D 2 )R 60 R 61 , 35 NR 60 NR 61 R 62 and ONR_6QR61' wherein D l s D 2 , D 3 and D 4 independently have the meaning of D as previously defined, and R 0 , R^ and Rg 2 independently have the meaning of R β as previously defined or any two or more of R βQ , R^ and R β2 form part of a saturated or unsamrated cyclic, bicyclic or fused ring system as defined below, or Rι 2 and Rι 3 together are selected from the group consisting of =O, =S, =NOR 60 , =NR 60 , -OQO-, -SQS- and -SQO-, wherein Q is optionally substituted (Cι-Cι 2 )alkylidene as defined below and R β0 is as previously defined; selected from the group consisting of wherein R 2 o3 and R 2 o3* independently have the meaning of R^ as previously defined, R 14 * and R 4 ** are independently selected from the group consisting of hydrogen, R 20 as previously defined, CF 3 , C(D*)OR4o, C(D*)SR4 0 and C(D*)NR4oR4i, wherein R4 0 and R41 independently have the meaning of R 21 and R 22 as previously defined or R40 and R4 form part of a samrated or unsamrated cyclic, bicyclic or fused ring system as defined below, R 14 is selected from the group consisting of F, Cl, Br, I, R 14 * as previously defined and R 2 QO as previously defined, R 17 and R17* independently have the meaning of R β as previously defined, D* has the meaning of D as previously defined, Z is a saturated or unsaturated (C 2 -C 4 )alkylidene radical which is optionally substituted with one or more groups selected from F, Cl, Br, I and R w * as previously defined, Z* is a samrated or unsaturated (C -C3)alkylidene radical which is optionally substimted with one or more groups selected from F, Cl, Br, I and R i * as previously defined, M ! is selected from the group consisting of OR 15 , SR 1 5 and NR 5R 7, wherein R15 is selected from the group consisting of: Px as previously defined, Rβ as previously defined, and a glycosyl radical which is derived from a synthetic or naturally occurring aldose, ketose, deoxyaldose, deoxyketose, aminoaldose, aminoketose or an oligosaccharide thereof, and R 7 is as previously defined, or R 5 and R J7 together form a samrated or unsamrated cyclic, bicyclic or fused ring system as defined below, M and M* are independently selected from the group consisting of M as previously defined, OCN, SCN, Y'R 2 , Y* and N=CR 30 R 3 ι, wherein Y', Y* and R 2 are as defined below, and R 30 and R 31 independently have the meaning of R 2 Q as previously defined, M 2 is selected from the group consisting of R 1 * as previously defined, -CR 30 *=Y** and -CR 30 *=NRι 7 *, where Y** is as defined below, R 30 * has the meaning of R 2 Q as previously defined, and R 17 * is as previously defined, Rι 8 and R19 independently have the meaning of R 2Q as previously defined or R i8 and R19 together form part of a samrated or unsamrated cyclic, bicyclic or fused ring system as defined below, and R 18 * and R 19 * together form part of a samrated or unsamrated cyclic, bicyclic or fused ring system as defined below; V is selected from the group consisting of Y'R 2 , Y* and C(R 3Q )=Y**, wherein Y' is selected from the group consisting of O O ' o- — S-N— — N=N— -N=N — -N=N— + + R 50 O o 0 o II II II II — S-N— -N— S — -N— S — II I I I II -o-s— II O R50 R50 R50O o o o o o II II —s-o— — s-s— —o-s— — s-o— II II o o o 0 o — S— S— — S-S— — P-N— — O-P-N— O R51O R50 R51 R50 0 0 0 o II II II II — N-P— — N-P-O— — P-O- — O— P— I I I I I I R 50 OR 51 R50OR51 0R 51 0R 51 O O O o II II II II — P— N — — N— P — — P-O— — O— P — I I I I I I and R51O R50 R50OR51 Rδ 2 Rδ 2 O II — 0— P-O— . I OR51 wherein R 50 has the meaning of Rg as previously defined, R 5i has the meaning of R 5 as previously defined and R 52 has the meaning of R 2 o as previously defined, or R 50 and R 51 together form part of a samrated or unsamrated cyclic, bicyclic or fused ring system as defined below, and R 2 has the meaning of R as previously defined, Y* is selected from the group consisting of R33 — N— N-R 2 * — N-N=C — N-0-R 2 * — O— N-R 2 * I I I R I Δ I R50 R51 R50 M R50 R50 R114* — P==D* ' , wherein D* and D** independently have the meaning of D as 114** previously defined; R114*, R114**, Rn 5 and R117* have the meaning of R14*, R14**, R15 and R17* respectively, as previously defined; R50 and R51 are as previously defined or R 5 o and R 5 together form part of a samrated or unsamrated cyclic, bicyclic or fused ring system as defined below; R 2 * is selected from the group consisting of R 2 as previously defined, S(O) z ORι 20 and S(O) Z NRI 2 QRI 2 I , wherein z is 1 or 2; R 33 and R 3 4 are independently selected from the group consisting of hydrogen and R 2Q as previously defined, or R 33 and R 34 together form a saturated or unsaturated cyclic, bicyclic or fused ring system as defined below, and Rι 20 and Rι 2 ι independently have the meaning of R 20 as previously defined, or Rι 20 and R121 together form a samrated or unsamrated cyclic, bicyclic or fused ring system as defined below, R 3 0 is as previously defined, and Y** is selected from =N-NRn 5 R 117 and =N-OR 115 , wherein Rn 5 and Rn 7 have the meamng of R 5 and Rg respectively, as previously defined, or Rll5 and R117 together form a samrated or unsaturated cyclic, bicyclic or fused ring system as defined below, and wherein any group selected from R i s R , R 2 , R 2 *, R 9 , R n , R 12 , R50 and R 51 may, together with any other group selected from R R j *, R 2 , R 2 *, R 9 *, R 0 , Rn, R12, R 50 and R 5 ι form one or more samrated or unsamrated cyclic, bicyclic or fused ring system(s) as defined below, -^N-0 and wherein any tertiary amino nitrogen atom may be replaced by the group and, where the sequence W'-(A') n .-B'-(A'*) m .-V' contains a grouping of three heteroatoms together, one atom of those three heteroatoms is oxidised sulfur in the form of S(O) or S(O) 2 , or oxidised phosphorus in the form of P(O), or the three heteroatoms comprise two nitrogen atoms which form part of a heterocycle, provided that the sequence W'-(A , ) n , -B , -(A , *) m -V' does not contain two oxygen atoms together or three sulfur atoms together; and wherein (a) when W is Rι*X* wherein X* is NR 0 , and V is Y* wherein Y* is wherein R 8 ι is selected from the group consisting of hydrogen, -Rκχ ) H, -RIOOC(O)ORIOI , -RιooC(O)NR 10 ιRιo 2 , -RιooNRι 0 2C(O)Rιoo* and wherein Rioi and RIQ 2 are independently selected from the group consisting of hydrogen, optionally substituted (Cι-Cιg)alkyl, optionally substituted (C 3 -Cιg)cycloalkyl, optionally substituted (C 3 -Cι 8 )cycloalkyl-(C -Cι 8 )alkyl, optionally substituted (C 6 -C 2 4)aryl, optionally substituted (C 7 -C 25 )aralkyl, optionally substimted (C -Cι 8 )alkenyl, optionally substimted (C 8 -C 2 g)-aralkenyl, optionally substimted (C 2 -C 8 )-alkynyl, optionally substimted (C 8 -C 2 g)- aralkynyl and optionally substimted heterocyclic, and wherein RIQO and R oo* are independently divalent radicals derived from a member selected from the group consisting of (Cι-Cιg)alkyl, (C 3 -Cι 8 )cycloalkyl, (C 3 -Cι 8 )cycloalkyl(C r C 18 )alkyl, (C 6 -C 24 )aryl, (C 7 -C 25 )aralkyl, (C 2 -Cι 8 )alkenyl, (C 8 -C 26 )aralkenyl, (C 2 -Cι 8 )- alkynyl, (Cg-C 2 g)aralkynyl and heterocyclic, any of which may be optionally substituted as defined below, and R 8 o is selected from the group consisting of R as previously defined and a solubilising and/or protecting group Px which is labile in vivo, then at least one of the following applies: (i) R 50 is a group Rs 3 , wherein R 53 is selected from the group consisting of C(D*)OR 2 ι*, C(D*)NR 2 ι*R 22 *, C(D*)SR 21 *, C(D*)R 55 , CF 3 , R 55 and a solubilising group Px which is labile in vivo, wherein D* has the meaning of D as previously defined, R 2 ι* and R 22 * have the meaning of R 2 ι and R 22 respectively, as previously defined, and wherein R55 is selected from the group consisting of optionally substituted (C r C 18 )alkyl(C 6 -C 24 )aryl, optionally substimted (C 2 -Cι 8 )alkenyl(C 6 -C 24 )aryl, optionally substimted (C 2 -Cι 8 )- alkynyl(C 6 -C 24 )aryl, optionally substimted (C 3 -C 18 )cycloalkyl- (C 2 .C 18 )alkenyl, optionally substimted (C 3 -Cι 8 )cyclo- alkyl(C 2 -C 18 )alkynyl, optionally substimted (C 3 -C 18 )cycloalkyl- (Cg-C24)aryl, optionally substimted acyl(C6-C 24 )aryl, optionally substimted heterocyclic(Cι-Cι 8 )alkyl, optionally substimted hetero- cyclic(C 2 -Cι 8 )alkenyl, optionally substituted heterocyclic- (C 2 -Cι 8 )alkynyl and optionally substituted heterocyclic(C 2 -Cιg)- (C 6 -C 24 )aryl, and n', m\ Ri*, Rι 0 , A', A'*, R 5J and R 2 * are as previously defined, (ii) one of R 2 * and R51 is a group R54, wherein R54 is selected from the group consisting of R55*, C(D*)NR 2 ι*R 2 2*, C(D*)OR 55 *, C(D*)R 55 *, C(D*)SR 2 ι*, CF 3 , S(O) z ORι 20 , S(0) z NR 12 oRi2i. and a solubilising group Px which is labile in vivo, wherein z is 1 or 2 and R 20 and Rι are as previously defined or Rι 20 and Rι together form a saturated or unsamrated cyclic, bicyclic or fused ring system as defined below, and wherein R 2 * and R2 2 * have the meaning of R 2 ι and R 22 respectively, as previously defined, and R55* has the meaning of R55, as previously defined, and n', m', Ri*, RI Q , A', A'*, R 50 and the other of R 2 * and R51 are as previously defined, (iii) at least one A' or A'* is selected from the group consisting of CR112R13, CRι 2 Rιi3, CRn 2 Rι 3 * and CRι 2 *Rn 3 , wherein Rn 2 and Rn 3 are independently selected from the group consisting of R55 as previously defined, C(D)OR 2! *, C(D)SR 2 ι*, C(D)NR 2 ι*R 22 *, F, Cl, Br and I, wherein R 2 ι* and R 22 * have the meaning of R 2 and R 22 respectively, as previously defined, and D, n', m', R *, R 2 *, Rι 0 , Rn > Rι 2 , Rι 2 *, Rι 3 , R13*, R50 and R51 are as previously defined, (iv) Ri* is selected from the group consisting of optionally substituted (C 2 -Cι 8 )alkenyl, optionally substimted (C 2 -C 18 )alkynyl, optionally substimted (C 3 -Cι 8 )cycloalkyl(C 2 -Cι 8 )alkenyl, optionally substimted (C 3 -Cι 8 )cycloalkyl(C 2 -Cι 8 )alkynyl, optionally substimted (C 6 -C 24 )aryl- (C 2 -Cι 8 )alkenyl, optionally substimted (C 6 -C 24 )aryl(C 2 -Cι 8 )alkynyl, optionally substimted (C 2 -Cι 8 )acyl, wherein the optional substituent is other than amino, optionally substimted (C 6 _C 2 )aryl(C 2 -C g)acyl, optionally substimted heterocyclic(Cι .Chalky 1, optionally substimted heterocyclic(C 2 -Cι 8 )alkenyl, optionally substimted heterocyclic(C 2 -Cι 8 )alkynyl, C(O)OR 90 , C(O)NR 9 ιR 92 , CF 3 , S(O) z OR 20 , S(O) z NR 20 Rι 2 and a solubilising group Px which is labile in vivo, wherein z is 1 or 2 and R 120 and R i21 are as previously defined, wherein R 90 is selected from the group consisting of (C 3 -Cι 8 )cycloalkyl, (C 3 -Cι 8 )cycloalkyl(C r Cι 8 )alkyl, heterocyclic, (C 2 -Chalky 1- heterocyclic, (C 6 -C 24 )aryl, (C 6 -C 24 )aryl(Cι-Cι 8 )alkyl and (Cg-C 24 )aryl(C 1 -C 18 )alkylheterocyclic , and wherein R 91 and R 92 are independently selected from the group consisting of optionally substituted (C 2 -C 8 )alkenyl, optionally substituted (C 2 -Cι 8 )alkynyl, optionally substimted (C 3 -Cι 8 )cycloalkyl, optionally substimted (C 3 -Cιg)cycloalkyl- (Cι-Cι )alkyl, optionally substituted (C 3 -Cι 8 )cycloalkyl- (C 2 -Cι 8 )alkenyl, optionally substituted (C 3 -Cι 8 )cycloalkyl- (C 2 -Cιg)alkynyl, optionally substituted (C 6 -C 24 )aryl- (C -Cι 8 )alkenyl, optionally substituted (C 6 -C 2 4)aryl- (C 2 -Cι 8 )alkynyl, optionally substituted (C 2 -C 18 )acyl, optionally substituted (Cg-C 24 )aryl(C 2 -Cι 8 )acyl, optionally substituted heterocyclic, optionally substituted heterocyclic(Cι-Cι 8 )alkyl, optionally substimted heterocyclic(C 2 -Cι 8 )alkenyl, and optionally substituted heterocyclic(C 2 .Cι 8 )alkynyl, or R 9 and Rg 2 together form a samrated or unsamrated cyclic, bicyclic or fused ring system as defined below, and m' , n', A', A'*, R 2 *, R 50 , R 51 and Rι 0 are as previously defined, (v) a group selected from Rj, Ri*, R 2 , R 2* , R 9 , Rn, R J , R 50 and R 5 ι, taken together with another group selected from Ri, Ri*, R 2 , R 2* , R 9 *, Rι 0 , Rn, R l2 , R 50 and R 51 is selected from the group consisting of -C(O)- and optionally substimted methylene; — N— N-R 2 * I I (b) when W is R 2* X* wherein X* is NR 10 , and V is Y* wherein Y* is 50 51 and B' is selected from -CH(OH)- and -C(O)- then at least one of the following also applies when one of the conditions (i) to (iv) defined above in (a) applies: (vi) n' > 1, (vii) n' = 0, (viii) m' > 1, (ix) m' = 0, (x) R 50 and R 5 together form part of a samrated or unsamrated cyclic, bicyclic or fused ring system as defined below, (xi) R 50 is a group R 5 g, wherein R 56 is selected from the group consisting of C(D*)OR 2!* , C(D*)NR 2 ι * R 22* , C(D*)SR 2 ι * , C(D*)R 55 and a solubilising and/or protecting group Px which is labile in vivo, wherein R 21* and R 22* are as previously defined, and (xii) n' = m' = 1 and A'* is other than -CH 2 -, R 14 * Ri7 Ri4 * and (c) when B' is selected from — p I — — o — — s — — N ' — — N ' — Rl4* — C— I and 14 , wherein R , R14* and R i7 are as previously defined, then at least one group selected from R 2 or R 2 *, Rn, Rι 2 , R50 and R 5 ι together with another group selected from R or R *, Rι 0 , Rn and Rι 2 forms a saturated or unsaturated cyclic, bicyclic or fused ring system as defined below, said ring being substimted with at least one polar group selected from =O, =S, OH, SH, NHR10* and C(O)OH, wherein Rι 0 * has the meaning of Rι 0 as previously defined, said polar group being sterically capable of being located within the compound of formula (I) not more than 5 Angstrom units from the P, O, S, N or C atom of group B, provided that when W is R 2 *X* and X* is NH and V is Y* wherein Y* is wherein Ri* is other than H and R 71 and R 7 are independently selected from the group consisting of H, (C r C6)alkyl, optionally substimted phenyl, optionally substimted naphthyl, optionally substimted phenyl(Cι-C 2 )alkyl and optionally substimted naphthyl- (Cι~C 2 )alkyl, and when (a) B' is -CH(OH)- and (A') n is -CH(R 73 )- wherein R 73 is selected from the group consisting of (C r C 6 )alkyl optionally substimted with 1-5 fluorine atoms, (C 3 -C 6 )alkenyl, (C r C 6 )alkoxy-CH 2 -, (CH 2 ) p phenyl, (CH 2 ) p naphthyl, (CH 2 ) p. (C 5 -C 6 )cycloalkyl and (CH 2 ) p indolyl, wherein said (CH 2 ) n phenyl, (CH 2 ) n naphthyl, (CH 2 ) n (C 5 -C 6 )cycloalkyl and (CH 2 ) π indolyl are optionally substimted with nitro, halogen, (C r C 4 )alkyl, (C r C 4 )alkoxy or (C r C 4 )alkylthio and wherein p is 0, 1 or 2, then (A'*) m . is other than OHO I II — CH 2 -C-C- wherein R 74 has the meaning of R 73 as previously defined, and R 74 when OH (b) B' is — C— wherein R 74 has the meaning of R 73 as previously defined and R 74 H H H (A . is -c-c-c- wherein R 73 is as previously defined, then (A'*) m - is R 73 OH H other than -C(O)-, and when H H H H I I I I (c) B' is -C(O)- and (A') n - is -c— c— c— c— wherein R 73 is as previously R 73 OH H OH defined, then m' is other than 0. As used herein, the term " (C -Chalky 1" includes within its meaning straight and branched chain alkyl groups having from 1 to 18 carbon atoms. Examples of such groups are methyl, ethyl, propyl, isopropyl, butyl, isobutyl, sec-butyl, tert-butyl, amyl, isoamyl, sec-amyl, 1,2-dimethylpropyl, 1,1-dimethyl-propyl, hexyl, 4-methylpentyl, 1-methylpentyl, 2-methylpentyl, 3-methylpentyl, 1,1-dimethylbutyl, 2,2-dimethylbutyl, 3,3-dimethylbutyl, 1,2-dimethylbutyl, 1,3-dimethylbutyl, 1,2,2-trimethylpropyl, 1,1,2-trimethylpropyl, heptyl, 5-methylhexyl, 1-methylhexyl, 2,2-dimethylpentyl, 3,3-dimethylpentyl, 4,4-dimethylpentyl, 1,2-dimethylpentyl, 1,3-dimethylpentyl, 1,4-dimethyl-pentyl, 1,2,3-trimethylbutyl, 1,1,2-trimethylbutyl, 1,1,3-trimethylbutyl, octyl, 6-methylheptyl, 1-methylheptyl, 1,1,3,3-tetramethylbutyl, nonyl, 1-, 2-, 3-, 4-, 5-, 6- or 7-methyl-octyl, 1-, 2-, 3-, 4- or 5-ethylheptyl, 1-, 2- or 3-propylhexyl, decyl, 1-, 2-, 3-, 4-, 5-, 6-, 7- or 8-methylnonyl, 1-, 2-, 3-, 4-, 5- or 6-ethyloctyl, 1-, 2-, 3- or 4-propylheptyl, undecyl, 1-, 2-, 3-, 4-, 5-, 6-, 7-, 8- or 9-methyldecyl, 1-, 2-, 3-, 4-, 5, 6- or 7-ethylnonyl, 1-, 2-, 3-, 4- or 5-propyloctyl, 1-, 2- or 3-butylheptyl, 1-pentylhexyl, dodecyl, 1-, 2-, 3-, 4-, 5-, 6-, 7-, 8-, 9- or 10-methylundecyl, 1-, 2-, 3-, 4-, 5-, 6-, 7- or 8-ethyldecyl, 1-, 2-, 3-, 4-, 5- or 6-propylnonyl, 1-, 2-, 3- or 4-butyloctyl, 1- or 2-pentylheptyl, tridecyl, tetradecyl, hexadecyl, octadecyl and the like. Typically an alkyl group is (C a -C b )alkyl, in which a is selected from a value presented in the column headed "a" in Table A below at one of entries 1-17, and b has one of the values presented in the column headed "b" at that entry. Table A As used herein, the term "(C 2 -C ι 8 )alkenyl" includes within its meaning ethylenically mono-, di- or poly-unsaturated alkyl groups having from 2 to 18 carbon atoms, and may be straight-chain or branched. Examples of such alkenyl groups are vinyl, allyl, 1 -methyl vinyl, 1-propenyl, 1-butenyl, 2-butenyl, 3-butenyl, 1,3-butadienyl, 2-methyl-l-propenyl, 2-methyl-2-propenyl, 1-pentenyl, 2-pentenyl, 3-pentenyl, 4-pentenyl, 1,3-pentadienyl, 2,4-pentadienyl, 1,4-pentadienyl, 3-methyl-2-butenyl, 1-hexenyl, 2-hexenyl, 3-hexenyl, 1,3-hexadienyl, 1,4-hexadienyl, 2-methylpentenyl, 1-heptenyl, 3-heptenyl, 1-octenyl, 1,3-octadienyl, 1-nonenyl, 2-nonenyl, 3-nonenyl, 1-decenyl, 3-decenyl, 1-undecenyl, oleyl, linoleyl and linolenyl. Typically an alkenyl group is (C a -C b )alkenyl, in which a is selected from a value presented in the column headed "a" in Table A above at one of entries 2-17, and b has one of the values presented in the column headed "b" at that entry. As used herein, the term "(C 2 -Cι 8 )alkynyl" includes within its meamng mono-, di- and poly-acetylenically unsaturated alkyl groups having from 2 to 18 carbon atoms, and may be straight-chain or branched. Examples of such alkynyl groups are ethynyl, propynyl, n-butynyl, n-pentynyl, 3-methyl-l-butynyl, n-hexynyl, methyl-pentynyl and (C 7 -Cι 2 )alkynyl. Typically an alkynyl group is (C a -C b )alkynyl, in which a is selected from a value presented in the column headed "a" in Table A above at one of entries 2-17, and b has one of the values presented in the column headed "b" at that entry. As used herein, the term "(C 3 -Cι 8 )cycloalkyl" refers to otionally unsamrated mono-, di- or polycyclic alkyl groups having from 3 to 18 carbon atoms. Examples of such groups include cyclopropyl, cyclobutyl, cyclopentyl, cyclopentenyl, cyclopentadienyl, cyclohexyl, cyclohexenyl, cyclohexadienyl, cycloheptyl, cycloheptenyl, cycloheptadienyl, cycloheptatrienyl, cyclooctyl, cyclooctenyl, cyclooctadienyl, cyclooctatrienyl, cyclooctatetraenyl, cyclononyl, cyclodecyl, cycloundecyl, cyclododecyl, (C 9 _Cι 2 )cycloalkynyl, bicyclo[2.2.1]heptanyl, bicyclo[2.2.1]heptenyl, bicyclo[2.2.1]- heptadienyl, bicyclo[2.2.2]octanyl, bicyclo[2.2.2]octenyl, bicyclo[3.3.1]nonyl, bicyclo- [3.1.0]hexyl, bicyclo[4.1.0]heptyl, bicyclo[3.2.1]octyl, bicyclo[3.3.0]octyl, bicyclo- [3.3.0]octenyl, bicyclo[3.3.1]nonyl, bicyclo[4.4.0]decyl, adamantyl, tricyclo[5.2.1.0 2 ' 6 ]decyl and the like. Typically a cycloalkyl group is (C a -C b )cycloalkyl, in which a is selected from a value presented in the column headed "a" in Table A above at one of entries 3-17, and b has one of the values presented in the column headed "b" at that entry. As used herein, the term "(C 3 -Cι 8 )cycloalkyl(Cι-C 8 )alkyl" refers to a (Cι-C 8 )alkyl group as defined above, substimted with a (C 3 -Cι 8 )cycloalkyl group as defined above. Examples of cycloalkylalkyl groups include cycloalkyl-loweralkyl groups, such as cycloalkylmethyl, cycloalkylethyl, cycloalkylpropyl, cycloalkylbutyl, cycloalkylisopropyl, cycloalkylisobutyl, cycloalkylpentyl and cycloalkylhexyl, wherein the cycloalkyl is as exemplified in the preceding paragraph. As used herein, the term "(C 3 -Cι )cycloalkyl(C 2 -C 8 )alkenyl" refers to a (C 2 -Cι 8 )alkenyl group as defined above, substimted with a (C 3 -C 8 )cycloalkyl group as defined above. Examples of cycloalkylalkenyl groups include cycloalkyl-loweralkenyl groups, such as cycloalkylethenyl, cycloalkylpropenyl, cycloalkylbutenyl, cycloalkylisobutenyl, cycloalkylpentenyl and cycloalkylhexenyl, wherein the cycloalkyl is as exemplified above under "(C 3 -C 8 )cycloalkyl". As used herein, the term "(C 3 -Cι 8 )cycloalkyl(C 2 -Cι 8 )alkynyl" refers to a (C 2 -Cι 8 )alkynyl group as defined above, substituted with a (C 3 -C 18 )cycloalkyl group as defined above. Examples of cycloalkylalkynyl groups include cycloalkyl-loweralkynyl groups, such as cycloalkylethynyl, cycloalkylpropynyl, cycloalkylbutynyl, cycloalkylpentynyl and cycloalkylhexynyl, wherein the cycloalkyl is as exemplified above under " (C 3 -C 1 8 )cycloalkyl " . As used herein, the term "(Cg-C^aryl" refers to single, polynuclear, conjugated and fused residues of aromatic hydrocarbons having from 6 to 24 carbon atoms. Examples of such groups are phenyl, biphenyl, terphenyl, quaterphenyl, naphthyl, tetrahydronaphthyl, acenaphthyl, anthracenyl, dihydroanthracenyl, benzanthracenyl, dibenzanthracenyl, phenanthrenyl, fluorenyl, pyrenyl, indenyl, indanyl, azulenyl, chrysenyl and the like. In all cases, any available position of the fused or conjugated bicyclic system can be used for attachment to the remainder of the molecule of formula (I). Typically an aryl group is (C a -C b )aryl, in which a is selected from a value presented in the column headed "a" in Table B below at one of entries 1-18, and b has one of the values presented in the column headed "b" at that entry. Table B As used herein, the term "(C 6 -C 24 )aryl(Cι-Cι 8 )alkyl" refers to a (C r Cι 8 )alkyl group substimted with one or more (C 6 -C 24 )aryl groups as previously defined. Examples of such groups are aryl-loweralkyl groups such as arylmethyl, arylethyl, arylisopropyl, arylpropyl, arylbutyl, arylisobutyl, arylpentyl and arylhexyl, wherein the aryl is as exemplified in the preceding paragraph, such as benzyl, diphenylmethyl, 2-phenylethyl, 1-phenylethyl, naphthylmethyl, 3-phenylpropyl, triphenylmethyl, 1,3-diphenylpropyl, 2- or 3-β-naphthylpropyl, 2-benzyl-propyl and the like. As used herein, the term "(C 7 -C 25 )aralkyl" refers to an alkyl group substimted with an aryl group, wherein the total number of carbon atoms in the aryl-substimted alkyl group is from 7 to 25. Optional substituents for (C 7 -C 25 )aralkyl are as defined below with respect to (C 6 -C 24 )aryl(Cι-Cι 8 )alkyl. As used herein, the term "(C 6 -C 24 )aryl(C r Cι 8 )alkenyr' refers to a (C r Cι 8 )alkenyl group substituted with one or more (C 6 -C 24 )aryl groups as previously defined. Examples of such groups are aryl-loweralkenyl groups such as arylethenyl, arylpropenyl, arylbutenyl, arylisobutenyl, arylpentenyl and arylhexenyl, wherein the aryl is as exemplified above under "(C 6 -C 24 )aryl" such as styryl, cinnamyl, 2-naphthylethenyl, l-phenyl-2-methyl-l-propenyl, 2-phenyl-2-butenyl and the like. As used herein, the term "(C 8 -C 26 )aralkenyl" refers to an alkenyl group substimted with an aryl group, wherein the total number of carbon atoms in the aryl- substimted alkenyl group is from 8 to 26. Optional substituents for (C 8 -C 26 )aralkenyl are as defined below with respect to (C 6 -C 2 )aryl(C 2 -Cι )alkenyl. As used herein, the term "(C 6 -C 24 )aryl(C r Cι 8 )alkynyl" refers to a (C r C 18 )alkynyl group substimted with one or more (C 6 -C 24 )aryl groups as previously defined. Examples of such groups are aryl-loweralkenyl groups such as arylethenyl, arylpropenyl, arylbutenyl, arylisobutenyl, arylpentenyl and arylhexenyl, wherein the aryl is as exemplified above under "(C6-C24)aryl" such as phenylethynyl and the like. As used herein, the term "(C 8 -C26)aralkynyl" refers to an alkynyl group substimted with an aryl group, wherein the total number of carbon atoms in the aryl- substimted alkynyl group is from 8 to 26. Optional substituents for (C 8 -C 2 6)aralkynyl are as defined below with respect to (C 6 -C 2 4)aryl(C 2 -Cιg)alkynyl. As used herein, the term "(Cι-Cιg)acyl" refers to a group R 30 oC(O)- or R 300 C(S)-, wherein R 300 is selected from the group consisting of hydrogen, (C r C 18 )alkyl, (C 2 -Cι 8 )alkenyl, (C 2 -Cι 8 )alkynyl, (C 3 -C 18 )cycloalkyl (C 3 -Cι 8 )cycloalkyl- (C r Cι 8 )alkyl, (C 3 -Cι 8 )cycloalkyl(C 2 -C 18 )alkenyl, (C 3 -Cι 8 )cycloalkyl(C 2 -Cι 8 )alkynyl, (C 6 -C 24 )aryl, (C 6 -C 24 )aryl(C r Cι 8 )alkyl, (C 6 -C 24 )aryl- (C 2 -C 8 )alkynyl, heterocyclic, heterocyclic(C r C 8 )alkyl, heterocyclic(C 2 -Cι 8 )alkenyl, and heterocyclic(C 2 -Cι 8 )alkynyl. Typically an acyl group is (C a -C b )acyl, in which a is selected from a value presented in the column headed "a" in Table A above at one of entries 1-17, and b has one of the values presented in the column headed "b" at that entry. Examples of acyl groups include loweralkylcarbonyl such as formyl, acetyl, propionyl, butyryl; loweralkenylcarbonyl such as pivaloyl, acryloyl, vinylacetyl, crotonoyl, 3-pentenoyl, 4-pentenoyl; and loweralkynylcarbonyl such as propioloyl, 2- butynoyl and 3-butynoyl, any of which may be substimted with cycloalkyl, aryl or heterocyclic as exemplified herein, as, for example, cyclopropylcarbonyl, cyclobutyl- carbonyl, cyclopentylcarbonyl, 1-cyclopentenylcarbonyl, cyclopentylacetyl, cyclohexyl- carbonyl, 1-cyclohexenylcarbonyl, 1,4-cyclohexadienylcarbonyl, cyclohexylacetyl, cyclo- hexenylacetyl, 1 ,4cyclohexadienylacetyl, bicyclo[2.2.1]hept-2-ylcarbonyl, bicyclo- [2.2. l]heptylacetyl, bicyclo[2.2.1]hepten-2-ylcarbonyl, bicyclo[2.2.2]oct-2-ylcarbonyl, bicyclo[2.2.2]octylacetyl, bicyclo[2.2.2]octyl-3-propionyl, bicyclo[2.2.2]octen-2-yl- carbonyl, bicyclo[3.3.1]non-9-ylcarbonyl, bicyclo[3.3.1]non-9-ylacetyl, bicyclononyl-3- propionyl, bicyclo[4.4.0]dec-2-ylcarbonyl, bicyclo[4.4.0]dec-2-ylacetyl, 1-adamantyl- carbonyl, 2-adamantylcarbonyl, 1-adamantylacetyl, 2-adamantylacetyl, tricyclo[5.2.1.0 2 - 6 ]dec-8-ylacetyl, benzoyl, phenylacetyl, diphenylacetyl, triphenylacetyl, 3-phenylpropionyl, dibenzylacetyl, α-naphthoyl, β-naphthoyl, α-naphthylacetyl, β- naphthylacetyl, indenylcarbonyl, indanylcarbonyl, phenanthrenylcarbonyl, 9-fluorenyl- carbonyl, pyrrolylcarbonyl, pyrrolylacetyl, furylcarbonyl, furylacetyl, thienylcarbonyl, thienylacetyl, pyrazinylcarbonyl, pyrazinylacetyl, pyrrolidinylcarbonyl, pyrrolidinyl- acetyl, pyridylcarbonyl, pyridylacetyl, pyrimidinylcarbonyl, pyrimidinylacetyl, piperidyl- carbonyl, piper idylacetyl, piperazinylcarbonyl, piperazinylacetyl, morpholinylcarbonyl, morpholinylacetyl, thiomorpholinylcarbonyl, thiomorpholinylacetyl, indolylcarbonyl, indolylacetyl, quinolylcarbonyl, quinolylacetyl, isoquinolylcarbonyl, isoquinolylacetyl, quinoxalinylcarbonyl, benzofuranylcarbonyl, benzofuranylacetyl, indolinylcarbonyl, . indolinylacetyl, 1 ,2,3 ,4-tetrahydroquinolylcarbonyl, 1 ,2,3 ,4-tetrahydroquinolylacetyl, 1,2,3,4-tetrahydroisoquinolylcarbonyl, 1,2,3,4-tetrahydroisoquinolylacetyl, cyclo- hexylacryloyl, cinnamoyl, styrylacetyl and phenylpropioloyl. As used herein, the term "heterocyclic" refers to any samrated or unsaturated 3- to 16-membered monocyclic, bicyclic or poly cyclic ring containing one or more heteroatom independently selected from oxygen, nitrogen and sulphur. The term "heterocyclic" includes any group in which a heterocyclic ring is fused to one or more benzene, naphthalene or cycloalkane rings. Sulfur-containing heterocyclics may be substimted at sulfur with one or two oxygen atoms. Examples of heterocyclics are pyridyl, thienyl, furyl, pyrrolyl, indolyl, pyridazinyl, perhydropyridazinyl, pyrazolyl, pyrazoldinyl, 2,3,5,6-tetrahydropyrazinyl, phthalazinyl, 1,2,3,4-tetrahydrophthalazinyl, perhydrophthalazinyl, thiazolyl, pyrimidinyl, quinolinyl, isoquinolinyl, benzofuranyl, benzothienyl, purinyl, quinazolinyl, phenazinyl, acridinyl, benzoxazolyl, benzothiazolyl, piperidyl, tetrahydrofuryl, imidazolyl, oxazolyl, thiazolidino, oxazolidinyl, isoxazolyl, isothiazolyl, isoxazolidinyl, imidazolidinyl, morpholinyl, pyrrolidinyl, pyrazolinyl, benzothienyl, benzisoxazolyl, benzoisothiazolyl, benzothiadiazolyl, tetrazolyl, triazolyl, thiadiazolyl, benzimidazolyl, pyrrolinyl, quinuclidinyl, 1,4-thioxanyl, 1,3-thioxanyl, aza- norbornyl, isoquinuclidinyl, pyranyl, furazanyl, azepinyl, lH-indazolyl, 2,3-dihydro-lH- indazolyl, quinoxalinyl, cinnolyl, 1,2,3,4-tetrahydrocinnolinyl, pteridinyl, naphthyridinyl, 4H-quinolizinyl, benz[e] indolyl, benzoxazinyl, benzoxadiazolyl, benzothiazinyl, benzotriazolyl, carbazolyl, β-carbolinyl, 1,2,3,4,5,6-hexahydro-β-carbolinyl, phenanthridyl, phenoxazinyl, phenothiazinyl, 1-azaacenaphthenyl, thiatriazolyl, oxadiazolyl, thiadiazolyl, chromanyl, thiachromanyl, isochromanyl, chromenyl, cyclo- hexa[b]pyrrolyl, cyclohepta[b]pyrrolyl, cyclohexa[d]pyrazolyl. cyclohexa[b]pyridyl, cyclohexa[b]pyrazinyl, cyclohexa[b]pyrimidinyl, cyclohexa[b]-l,4-oxazinyl, cyclohexa[b]- 1 ,4-thiazinyl, 2-imidazolinyl, 2,3-dihydropyridyl, piperazinyl, thiomorpholinyl, S,S- dioxo-thiomorpholinyl, indolinyl, S,S-dioxo-l,2,3-benzothiadiazolyl, S,S-dioxo-l,2- thioxanyl, S,S-dioxo-l,4-thioxanyl, isoindolinyl, 4,5,6,7-tetrahydroindolyl, 1,2,3,4-tetra- hydroquinolyl, 1,2,3,4-tetrahydroisoquinolyl, hexahydroquinolyl. hexahydroisoquinolyl, 1 ,2,3 ,4-tetrahydro-3 , 1-benzodiazinyl, 3 ,4-dihydro-3H-4, 1-benzoxazinyl, 3 ,4-dihydro-3H- 4,1 -benzothiazinyl, 2,3,4,5-tetrahydro-lH-5,l-benzazepinyl and 5,6-dihydro- phenanthridinyl and the like. Configurations which result in unstable heterocyclics are not included within the scope of the definition of "heterocyclic" or "samrated or unsamrated cyclic, bicyclic or fused ring system" . As used herein, the term "heterocyclic(C r C 18 )alkyl" refers to a (C r Cι 8 )alkyl group as previously defined, which is substimted with a heterocyclic group as previously defined. Examples of such groups are heterocyclic-loweralkyl groups such as hetero- cyclicmethyl, heterocyclicethyl, heterocyclicisopropyl, heterocyclicpropyl, heterocyclic- butyl, heterocyclicisobutyl, heterocyclicpentyl and heterocyclichexyl, wherein the hetero¬ cyclic is as exemplified in the preceding paragraph. As used herein, the term "heterocyclic(C -Cι 8 )alkenyl" refers to a (C r Cι 8 )alkenyl group as previously defined, which is substimted with a heterocyclic group as previously defined. Examples of such groups are heterocyclic-loweralkenyl groups such as heterocyclicethenyl, heterocyclicpropenyl, heterocyclicbutenyl, hetero- cyclicisobutenyl, heterocyclicpentenyl and heterocyclichexenyl, wherein the heterocyclic is as exemplified above under "heterocyclic". As used herein, the term "heterocyclic(Cι-Cι 8 )alkynyl" refers to a (Cι-Cι 8 )alkynyl group as previously defmed, which is substituted with a heterocyclic group as previously defmed. As used herein, the term "alkylidene" refers to divalent radicals derived from alkyl groups. Examples of such radicals are -CH 2 -, -CH 2 CH 2 -, -CH=CH-, -CH 2 CH 2 CH 2 -, -C(=CH 2 )CH 2 -, -CH 2 CH=CH-, -(CH 2 ) 4 -, -CH 2 CH 2 CH=CH-, -CH 2 CH=CHCH 2 - and -(CH 2 ) r - where r is 5-12. The term also refers to such radicals in which one or more of the bonds of the radical from part of a cyclic system, and to such radicals wherein one or more carbon atoms is replaced by O, S or NH. Examples of such radicals are groups of the structure and similar groups, including those shown above wherein any N or O atom is replaced by S. As used herein the term "samrated or unsaturated cyclic, bicyclic or fused ring system" refers to a stable cyclic system of up to 16 carbon atoms, wherein said ring system may contain: for 3- and 4-membered rings, one heteroatom; for 5-membered rings, one or two heteroatoms; for 6- and 7-membered rings, one to three heteroatoms; for 8- and 9-membered rings, from one to four heteroatoms; for 10- and 11-membered rings, from one to five heteroatoms; for 12- and 13-membered rings, from one to six heteroatoms; for 14- and 15-membered rings, from one to seven heteroatoms; and for 16-membered rings, from one to eight heteroatoms; the heteroatom(s) being independently selected from oxygen, nitrogen and sulphur; which ring system may be substimted with one or more substituents independently selected from: R 150 and a group T, where Rι 50 has the meaning of R 20 as previously defmed, and where T is selected from the group consisting of -F, -Cl, -Br, -I, -CF 3 , -CN, -NCO, -NCS, -OCN, -SCN, -N 3 , -OR' , -NR'R" , -NR'C(O)R", -NR'C^OR", -NR'^NR-'R' ", -NO 2 , -SR', -S(O)R', -S(O) 2 R\ -S(O)OR' , -S(O) 2 OR', -S(O)NR'R", -S(O) 2 NR'R", =O, =S, =N 2 , =NOH, =NOR' , -NR'OR', -CHO, -OC(O)R', -OC(O)OR', -OC(O)NR'R", -C(O)R', -C(O)OR', -C(O)NR'R", -OC(S)R' , -OC(S)OR', -OC(S)NR * R", -C(S)R', -C(S)OR', -C(S)NR'R" , -SC(O)R', -SC(O)OR', -SC(O)NR'R", -C(O)SR', -SC(S)R', -SC(S)OR', -SC(S)NR*R", -C(S)SR', -C(=NR')OR", -C(=NR')SR", -C(=NR , )NR"R"', -OS(O)R\ -OS(O) 2 R' , -OS(O)OR', -OS(O) 2 OR', -OS(O)NR'R", -OS(O) 2 NR'R* ' , NR'S^^NR' ^' " , -NR'S(O) 2 R", -NHC(=NH)NR' , -C(=NH)NR\ -P(O)(OR')R", -P(O)(SR')R", -P(O)(OR')OR", -P(O)(OR , )NR"R ', -P(O)R'R", -OP OXOR^R", -OP(O)(OR')OR" , -OP(O)(SR')OR", -OP^^R^NR' ^' " , -OP(O)R'R , and -B(OR')(OR"), wherein R', R" and R' " are independently selected from the group consisting of hydrogen, (C r Cι 8 )alkyl, typically (C r C 12 )alkyl; (C 3 -C 8 )cycloalkyl, typically (C 3 -Cι 2 )cycloalkyl; (C 3 -Cι 8 )cycloalkyl(C r Cι 8 )alkyl, typically (C 3 -Cι 2 )cyclo- alkyl(Cι-C 6 )alkyl; (C 6 -C 24 )aryl, typically (C 6 -Cι 6 )aryl; (C 6 -C 24 )aryl(C r Cι 8 )alkyl, typically (C 6 -Cι 0 )aryl(C r C 6 )alkyl; (C 2 -Cι 8 )alkenyl, typically (C 2 -Cι 2 )alkenyl; (C 6 -C 24 )- aryl(C 2 -C !8 )alkenyl, typically (C 6 -C 10 )aryl(C 2 -C 6 )alkenyl; (C 2 -Cι 8 )alkynyl, typically (C 2 -Cι 2 )alkynyl; (C 6 -C 24 )aryl(C 2 -C 18 )aralkynyl, typically (C 6 -Cι 0 )aryl(C r C 6 )alkynyl, heterocyclic, heterocyclic(C -Cι 8 )alkyl, typically heterocyclic(Cι-C 2 )alkyl, heterocyclic- (C 2 -Cι 8 )alkenyl, typically heterocyclic(C 2 -Cι 2 )alkenyl and heterocyclic(C 2 -C 18 )alkynyl, typically heterocyclic(C 2 -Cι 2 )alkynyl, and wherein R', R" and R' " may be optionally substimted with up to six groups independently selected from hydroxy, (C -Cg)alkoxy, (C r C 6 )aryloxy, (C r C 6 )thioalkoxy, (Cι-C 6 )thioaryloxy, (Cι-C 6 )alkoxy(C r C 6 )alkoxy, amino, (Cι-C 6 )alkylamino, di(C -C 6 )alkylamino, fluoro, chloro, bromo, iodo, carboxy, (Cι-Cg)alkoxycarbonyl, (Cι-C 6 )alkylaminocarbonyl and di(Cι-C 6 )alkylaminocarbonyl. Examples of samrated or unsamrated cyclic, bicyclic or fused ring systems are the heterocyclic and cyclic alkylidene groups exemplified above. As used herein, the term "optionally substimted (C -C 8 )alkyl" refers to a (CrCιg)alkyl group as defined above wherein one or more hydrogen atoms are replaced by one or more substitutents T as previously defined. Examples of substimted (C j -Chalky 1 groups include hydroxy-loweralkyl such as hydroxymethyl, hydroxyethyl and 3-hydroxypropyl; loweralkoxy-loweralkyl such as methoxy methyl, 2-methoxyethyl, 2,2-dimethoxyethyl and 3-methoxypropyl; aryloxy- loweralkyl such as phenoxymethyl, phenoxy ethyl, α-naphthyloxymethyl and β-naphthyl- oxyethyl; arylloweralkoxy-loweralkyl such as benzyloxymethyl, benzyloxyethyl and 3-benzyloxypropyl; halo-loweralkyl such as chloromethyl, trifluoromethyl, 2-fluoro-, 2-chloro-, 2-bromo- or 2-iodo-ethyl, 2,2,2-trifluoro-ethyl, 2,2,2-trichloro-ethyl, 3-chloro- propyl and 3-bromopropyl; amino-loweralkyl such as aminomethyl, 2-aminoethyl, 3- aminopropyl, 5-aminopentyl, dimethylaminomethyl, 2-dimethylaminoethyl and 3-phenyl- aminopropyl; carboxy-loweralkyl such as carboxymethyl, carboxyethyl and 3-carboxy- propyl; acylloweralkyl such as acylmethyl, acylethyl, acylpropyl, acylisopropyl, acyl- butyl, acylisobutyl, acylpentyl and acylhexyl wherein the acyl is as exemplified above under "(Cι-Cιg)acyl"; acyloxy-loweralkyl such as acetoxymethyl, acetoxyethyl, 2-acetoxypropyl, 3-acetoxypropyl, propionyloxyethyl and 3-propionyloxypropyl; lower- alkylcarbonylamino-loweralkyl such as acetylaminomethyl, acetylaminoethyl, 2-acetyl- aminopropyl, propionylaminomethyl and propionylaminoethyl; loweralkylaminocarbonyl- amino-loweralkyl, such as dimethylaminocarbonylaminoethyl; sulfonyl-loweralkyl such as methylsulfonyl-methyl, ethylsulfonyl-methyl, tert-butylsulfonyl-methyl, phenylsulfonylmethyl, phenylsulfonylethyl, 4-toluenesulfonylethyl and 4-toluenesulfonyl- methyl; cyano-loweralkyl such as cyanomethyl, 2-cyanoethyl, 2-cyanopropyl, 3-cyano- propyl, 2-cyanobutyl, 3-cyanobutyl and 4-cyanobutyl; oxo-loweralkyl such as 2-oxo- propyl, 2-oxo-butyl, 3-oxo-butyl, 2-, 3- or 4-oxo-pentyl and 2,4-dioxo-pentyl; and lower- alkyl groups substimted with two or more than different substitutents as exemplified above. As used herein, the term "optionally substimted (Cι-Cι 8 )alkenyl" refers to a (Cι-Cιg)alkenyl group as defined above wherein one or more hydrogen atoms are replaced by a substituent or substitutents T as previously defmed. As used herein, the term "optionally substimted (Cι-Cιg)alkynyl" refers to a (Cι-Cιg)alkynyl group as defined above wherein one or more hydrogen atoms are replaced by a substituent or substitutents T as previously defined. As used herein, the term "optionally substimted (C 3 -C 24 )cycloalkyl" refers to a (C 3 -C 2 )cycloalkyl group as defined above wherein one or more hydrogen atoms are replaced by a substituent or substitutents independently selected from R IV and T as previously defined, wherein R IV is selected from (Cι-Cιg)alkyl, (C 2 -Cι 8 )alkenyl, (C 2 -Cι 8 )alkynyl, (C 3 -Cι 8 )cycloalkyl, (C 3 -Cι 8 )cycloalkyl(C r Cι 8 )alkyl, (C 3 -Cι 8 )cyclo- alkyl(C 2 -Cι 8 )alkenyl, (C 3 -Cι 8 )cycloalkyl(C 2 -Ci 8 )alkynyl, (C 2 -Cι 8 )acyl, (C 6 -C 24 )aryl(C 2 _.Cι 8 )acyl, heterocyclic, heterocyclic(C r Cι 8 )alkyl, heterocyclic(C 2 - Cι 8 )alkenyl, and heterocyclic(C 2 -Cι 8 )alkynyl, and wherein R IV may be substituted with up to six groups independently selected from hydroxy, amino, (Cι-C 6 )alkoxy, (C r C 6 )alkoxy(Cι-C 6 )alkoxy, amino, (C r C 6 )alkylamino, di(C r C 6 )alkylamino, fluoro, chloro, bromo, iodo, carboxy, (Cι-C 6 )alkoxycarbonyl, (C r C 6 )alkylaminocarbonyl and di(C i -C 6 )alkylaminocarbony 1. As used herein, the term "optionally substimted (C 3 -C 24 )cyclo- alkyl(Cι-Cιg)alkenyl" refers to a (C 3 -C 24 )cycloalkyl(Cι-Cιg)alkenyl group as defined above which are substimted in the cycloalkyl group by a substituent or substitutents independently selected from the substituents defined above for (C 3 -C 24 )cycloalkyl, and/or substimted in the alkenyl group by one or more substituents T as previously defined. As used herein, the term "optionally substimted (C 3 -C 2 )cyclo- alkyl(Cι-Cι 8 )alkynyl" refers to a (C 3 -C 24 )cycloalkyl(C r Cι 8 )alkynyl group as defined above which are substituted in the cycloalkyl group by a substituent or substitutents independently selected from the substituents defined above for (C 3 -C 24 )cycloalkyl, and/or substituted in the alkynyl group by one or more substituents T as previously defined. As used herein, the term "optionally substimted (Cg-C^aryl" refers to a (Cg-C 2 4)aryl group as defined above wherein one or more hydrogen atoms are replaced by a substituent or substitutents independently selected from R v and T*, wherein T* is selected from the group consisting of -F, -Cl, -Br, -I, -CF 3 , -CN, -NCO, -NCS, -OCN, -SCN, -N 3 , -OR * , -NR'R", -NR'C(O)R", -NR'C(O)OR", -NR , C(0)NR"R , , \ -NO 2 , -SR' , -S(O)R' , -S(O) 2 R', -S(O)OR\ -S(O) 2 OR', -S(O)NR'R", -S(O) 2 NR'R", -NR' OR', -CHO, -OC(O)R' , -OC(O)OR\ -OC(O)NR'R", -C(O)R * , -C(O)OR * , -C(O)NR'R", -OC(S)R\ -OC(S)OR', -OC(S)NR * R", -C(S)R\ -C(S)OR' , -C(S)NR'R", -SC(O)R', -SC(O)OR' , -SC(O)NR*R", -C(O)SR', -SC(S)R\ -SC(S)OR' , -SC(S)NR'R", -C(S)SR * , -C(=NR')OR", -C(=NR')SR", -C(=NR')NR"R" ', -OS(O)R' , -OS(O) 2 R', -OS(O)OR', -OS(O) 2 OR', -OS(O)NR'R", -OS(O) 2 NR'R", NR'S(O) 2 NR"R'" , NR'S(O) 2 R", -NHC(=NH)NR', -C(=NH)NR', -OP(O)(OR')R", -OP(O)(OR * )OR" , OP(O)(SR')OR", -OP(O)(OR , )NR"R , M , -OP(O)R'R", and -B(OR')(OR"), wherein R', R" and R" ' are as defined above with respect to the substituent T; and wherein R v is selected from (Cι-Cιg)alkyl, (C 2 -Cι 8 )alkenyl, (C2-Cι 8 )alkynyl, (C 3 -Cι 8 )cycloalkyl, (C 3 -Cι 8 )cycloalkyl(C r Cι 8 )alkyl, (C 3 -Cι 8 )cycloalkyl(C 2 -Cι 8 )alkenyl, (C 3 -Cι 8 )cycloalkyl- (C 2 -Cι 8 )alkynyl, (C 2 -Cι 8 )acyl, (C 6 -C 24 )aryl(C 2 ..Cι 8 )acyl, heterocyclic, heterocyclic- (Cι-Cιg)alkyl, heterocyclic(C 2 -Cιg)alkenyl, and heterocyclic(C -C 8 )alkynyl, and wherein R v may be substimted with up to six groups independently selected from hydroxy, amino, (C r C 6 )alkoxy, (Cι-C 6 )aryloxy, (C r C 6 )thioalkoxy, (C r C 6 )thioaryloxy, (C r C6)alkoxy(Cι-C 6 )alkoxy, amino, (Cι-C 6 )alkylamino, di(C -C 6 )alkylamino, fluoro, chloro, bromo, iodo, carboxy, (C r C 6 )alkoxycarbonyl, (C r C 6 )alkylaminocarbonyl and di(Cι-C 6 )alkylaminocarbonyl. The term "optionally substimted (C6-C 24 )aryl" includes mono-, di- and poly substimted (Cg-C^aryl groups. Examples of substimted aryl groups are loweralkyl-aryl, loweralkenyl-aryl, aryl- loweralkyl-arylloweralkylcarbonyl-aryl, heterocyclic-aryl and heterocyclicloweralkyl-aryl wherein the aryl group is as exemplified above; halo-aryl such as 4-chlorophenyl, 2,4-dichlorophenyl, l-chloro-2-naphthyl and 4-chloro-l-naphthyl; hydroxy-aryl such as 2-hydroxyphenyl, l-hydroxy-2-naphthyl, 2-hydroxy-l-naphthyl, 2-hydroxy-8-naphthyl, 3,4,5-trihydroxyphenyl and 2,4,5-trihydroxyphenyl; loweralkoxyaryl such as 4-methoxy- phenyl, 3,4-dimethoxyphenyl, 2,4-dimethoxyphenyl and l-methoxy-2-naphthyl; carboxy- aryl such as 2-carboxy-phenyl, 2-carboxy-l-naphthyl, l-carboxy-2-naphthyl and 9- carboxy-2-anthracyl; acylaryl, wherein the acyl group is as exemplifed above under "(C r C 18 ) acyl", such as 4-formylphenyl, 4-acetylphenyl, 2-benzoylphenyl, 2-methoxycarbonyl-phenyl , 2-ethoxycarbonyl- 1 -naphthyl , 1 -methoxycarbonyl-2-naphthyl , 9-methoxycarbonyl-2-anthracy 1 , 2-carbamoyl-phenyl , 2-carbamoyl- 1 -naphthyl , 1 -carbamoyl-2-naphthyl , 4-dimethylaminocarbonyl-phenyl , 4-morpholinocarbonylphenyl , 4-(2-pyridylmethoxy)carbonyl-phenyl and 4-benzyloxycarbonyl-phenyl; nitro-aryl such as 4-nitrophenyl and 2,4-dinitrophenyl; amino- or (substituted amino)-aryl such as 4-amino- phenyl, 2,4-diaminophenyl, 4-dimethylaminophenyl, 4-anilinophenyl, 2-(2,6- dichloroanilino)-phenyl, 2,4-di-(benzyloxycarbonylamino)-phenyl and 4-(2-quinoline- carbonylamino)-phenyl; and cyano-aryl such as 4-cyanophenyl, as well as aryl groups substimted with two or more of the substituents exemplified above. As used herein, the term "optionally substituted (C 6 -C 24 )aryl(Cι-Cι 8 )alkyl" refers to a (C 6 -C 24 )aryl(Cι-Cι 8 )alkyl group as previously defined substituted in the aryl group with one or more substimtents defined above for (Cg-C^aryl and/or substimted in the alkyl group with one or more substimtents defined above for (Cι-Cι 8 )alkyl. Examples of such groups are (substimted aryl)-lower-alkyl such as (substituted aryl)methyl, (substituted aryl)ethyl, (substituted aryl)propyl, (substimted aryl)iso-propyl, (substimted aryl)butyl, (substimted aryl)pentyl and (substimted aryl)hexyl, aryl(substituted loweralkyl) such as phenyl(substituted loweralkyl), naphthyl(substituted loweralkyl), biphenyl(substimted loweralkyl), tetrahydronaphthyl (substimted loweralkyl), indenyl- (substimted loweralkyl) and indanyl (substimted loweralkyl), and (substimted aryl)- (substituted loweralkyl), wherein in each case substimted aryl is as exemplified above with respect to "optionally substimted (C 6 -C 24 )aryl" and (substimted loweralkyl) is as exemplified above with respect to "optionally substimted (Cι-Cι 8 )alkyl". As used herein, the term "optionally substimted (C 6 -C 24 )aryl(Cι-C 8 )alkenyl" refers to a (C 6 -C 24 )aryl(Ci-Ci 8 )alkenyl group as previously defmed substimted in the aryl group with one or more substimtents defmed above for (C 6 -C 24 )aryl and/or substimted in the alkenyl group with one or more substimtents defined above for (C -Cι 8 )alkyl. As used herein, the term "optionally substimted (C 6 -C 24 )aryl(Cι-C 8 )alkynyl" refers to a (C 6 -C 2 )aryl(Cι-Cι 8 )alkynyl group as previously defined substimted in the aryl group with one or more substimtents defined above for (C 6 -C 24 )aryl and/or substimted in the alkynyl group with one or more substimtents defined above for (Cι-Cι 8 )alkyl. As used herein, the term "optionally substituted (Cι-C 8 )acyl" refers to a (Cι-Cι 8 )acyl group as previously defmed which may be substimted with one or more groups selected from the substituents defined for (Cι-Cιg)alkyl, and includes within its meaning an acyl residue of a namrally occurring or synthetic amino acid or azaamino acid, or an acyl residue of a peptide chain containing 2-4 namrally occurring or synthetic amino acids and/or azaamino acids. Examples of substimted acyl groups include acyl residues of any of the namrally occurring or synthetic amino acids exemplified herein, hydroxy loweralkanoyl, lower- alkoxyloweralkanoyl, acetylloweralkanoyl, cyanoloweralkanoyl, carboxy loweralkanoyl, hydroxycarboxy loweralkanoyl, fluoroloweralkanoyl, chloroloweralkanoyl, bromolower- alkanoyl, thioloweralkanoyl, loweralkanethioloweralkanoyl, aminoloweralkanoyl, lower- alkylaminoloweralkanoyl , di-(loweralky lamino)loweralkanoyl , carbamoy lloweralkanoyl , loweralkoxy carbonyl, carbamoyl, loweralkylaminocarbonyl and di-(loweralkylamino)- carbonyl, where loweralkanoyl is an alkanoyl group of from 1 to 6 carbon atoms, for example formyl, acetyl, propionyl, butyryl, isobutyryl, pentanoyl and hexanoyl, and where loweralkyl signifies a (Cι-C 6 )alkyl group such as methyl, ethyl, n-propyl, iso- propyl, n-butyl, iso-butyl, sec-butyl, tert-butyl, n-pentyl, iso-pentyl, neo-pentyl and hexyl. As used herein, the term "optionally substimted heterocyclic" refers to a heterocyclic group as previosly defined wherein one or more hydrogen atoms may be replaced with a group selected from the substitutents defmed above with regard to optionally substituted (Cg-C 24 )aryl. Examples of substited heterocyclic groups include loweralkylheterocyclic, arylheterocyclic, aryloxyheterocyclic, loweralkoxyheterocyclic, oxo-heterocyclic, hydroxyheterocyclic, loweralkoxycarbonylheterocyclic and lower- alkanoy lheterocyclic . As used herein, the term "optionally substimted heterocyclic(C 1 -Cι 8 )alkyl" refers to a heterocyclic(C -Cι )alkyl group as previously defined substimted in the heterocyclic group with one or more substimtents defined above for heterocyclic and/or substituted in the alkyl group with one or more substitutents defined above for (Cι-Cι 8 )alkyl. Examples of such groups are (substimted heterocyclic)-lower-alkyl such as (substituted heterocyclic)methyl, (substituted heterocyclic)ethyl, (substimted heterocyclic)propyl, (substimted heterocyclic)iso-propyl, (substimted heterocyclic)butyl, (substimted heterocyclic)pentyl and (substimted heterocyclic)hexyl, heterocyclic(substituted loweralkyl) such as pyrrolyl(substimted loweralkyl), indolyl(substituted loweralkyl), quinolyl(substituted loweralkyl), tetrahydroquinolyl(substituted loweralkyl), pyridyl- (substimted loweralkyl), morpholinyl(substituted loweralkyl), piperidinyl(substituted loweralkyl), thiomorpholinyl(substituted loweralkyl), thienyl(substituted loweralkyl), furanyl(substituted loweralkyl), benzfuranyl(substituted loweralkyl), pyrrolidinyl- (substituted loweralkyl) and iso-quinolyl(substituted loweralkyl), and (substimted heterocyclic) (substimted loweralkyl), wherein in each case substimted heterocyclic is as exemplified above with respect to "optionally substimted heterocyclic" and (substimted loweralkyl) is as exemplified above with respect to "optionally substimted (C -C 8 )alkyl". As used herein, the term "optionally substimted heterocyclic(C 1 -Cι 8 )alkenyl" refers to a heterocyclic(Cι-Cι 8 )alkenyl group as previously defmed substimted in the heterocyclic group with one or more substimtents defmed above for heterocyclic and/or substimted in the alkenyl group with one or more substimtents defined above for (C r C 18 )alkenyl. As used herein, the term "optionally substimted heterocyclic(Cι-Cι 8 )alkynyl" refers to a heterocyclic(C r Cι 8 )alkynyl group as previously defined substimted in the heterocyclic group with one or more substimtents defined above for heterocyclic and/or substituted in the alkynyl group with one or more substitutents defmed above for (C r C 18 )alkynyl. As used herein, the term "optionally substituted alkylidene" refers to an alkylidene radical as previously defined, in which one or more hydrogen atoms is replaced by substituent(s) independently selected from the substituents defined above in connection with "optionally substimted (Cι " Cι 8 )alkyl". As used herein, the term "namrally occurring or synthetic amino acid" refers to a compound of the formula HN(R 40 ι)(CH(R 4 oo)) p COOH, wherein R4 00 and R 401 independently have the meaning of R 2 o as previously defined, and p is 1, 2 or 3, and wherein R 400 and R 401 , together with the carbon and nitrogen to which they are bound may together form a samrated or unsamrated cyclic, bicyclic or fused ring system. Examples of namrally occurring or synthetic amino acids include alanine, cyclohexylalanine, anthranilic acid, arginine, asparagine, aspartic acid, cysteine, β- phenylcysteine, cystine, glutamic acid, glutamine, glycine, cyclohexylglycine, tetrahydrofuranylglycine, histidine, homoserine, hydroxyproline, isoleucine, leucine, lysine, 4-azalysine, δ-hydroxylysine, methionine, norleucine, norvaline, ornithine, phenylalanine, 4-aminophenylalanine, 4-carboxyphenylalanine, 4-chlorophenylalanine, phenylglycine, 8-phenylserine, proline, serine, threonine, trans-3-hydroxyproline, trans-4- hydroxyproline, tryptophan, tyrosine, valine, indoline-2-carboxylic acid, 1,2,3,4-tetra- hydroisoquinoline-3-carboxylic acid, aminomalonic acid, aminomalonic acid monoamide, α-aminobutyric acid, α,7-diaminobutyric acid and α,β-diaminopropionic acid. Other amino acids, and peptides derived therefrom, are disclosed in J. S. Davies, ed., Amino Acids and Peptides, Chapman and Hall, London, 1985, the disclosure of which is incorporated herein by reference. As used herein, the term "residue of a namrally occurring or synthetic amino acid" refers to a group of the formula -N(R 40 ι)(CH(R 400 )) p C(O)-, wherein R^, R 401 and p are as defined above with regard to "namrally occurring or synthetic amino acid" . As used herein, the term "azaamino acid" refers to an amino acid in which a -CH(R 4 oo)- group has been replaced by a group -N(R 40 ι)-, wherein R 401 has the meaning of R 20 as previously defmed. Suitable pharmaceutically acceptable salts of the compound of formula (I) are, where the compound of formula (I) contains a basic nitrogen atom, acid addition salts of pharmaceutically acceptable inorganic acids such as hydrochloric, sulfuric, phosphoric, nitric, carbonic, boric, sulfamic, hydrobromic or hydriodic, or with pharmaceutically acceptable organic acids such as acetic, propionic, butyric, tartaric, maleic, hydroxymaleic, methylmaleic, fumaric, malic, citric, lactic, mucic, gluconic, glucoheptonic, glucaric, glucuronic, lactobionic, benzoic, naphthoic, succinic, oxalic, phenylacetic, methanesulphonic, ethanesulfonic, 2-hydroxyethanesulfonic, ethane-1,2- disulfonic, laurylsulfonic, toluenesulphonic, benzenesulphonic, naphthalene-2-sulfonic, salicylic, 4-aminosalicylic, sulphanilic, aspartic, glutamic, edetic, stearic, palmitic, oleic, lauric, pantothenic, tannic, ascorbic, valeric, gly colic, cinnamic, mandelic, 2- phenoxybenzoic, 2-acetoxybenzoic, embonic, nicotinic, isonicotinic, N- cyclohexylsulfamic or other acidic organic compounds, such as 2- or 3-phosphoglycerate and glucose-6-phosphate. Where the compound of formula (I) contains an acid group, suitable pharmaceutically acceptable salts of the compound of formula (I) are addition salts of pharmaceutically acceptable bases such as lithium, sodium, potassium, ammonium, magnesium, calcium and zinc salts, or salts formed with organic amines such as methylamine, dimethylamine, trimethylamine, ethylamine, diethylamine, triethylamine, N-methyl-N-ethylamine, mono-, bis- or tris-(2-hydroxyethyl)amine, 2-hydroxy-tert-butyl- amine, tris(hydroxymethyl)methylamine, N,N-dimethyl-N-(2-hydroxyethyl)-amine, tri-(2- hydroxyethyl)-amine, N-methyl-D-glucamine, or tributylamine. Compounds of formula I having acid and basic groups can also form internal salts. Other suitable salts are described, for example, in S. M. Berge, et al , "Pharmaceutical Salts" J. Pharm. Sci.. 66 1-19 (1977) which is incorporated herein by reference. The expression "prodrug" as used herein refers to a pharmaceutically acceptable derivative of a compound of formula (I) which is transformed into a compound of formula (I) after administration of the prodrug to a living animal or human, and which has enhanced stability, delivery characteristics and/or therapeutic value compared to the compound of formula (I) from which it derives. The expression "protecting group" as used herein refers to a group which may be used temporarily to modify a functional group, for example to prevent that functional group from being affected by, or from undesirably affecting the outcome of, a desired reaction involving another functional group in the molecule and/or to prevent premature metabolism of the compound of formula (I) after administration to a patient before the compound can reach the desired site of action. Suitable protecting groups are described, for example in Greene, T. W., Protective Groups in Organic Synthesis (John Wiley & Sons, New York, 1981) and McOmie, J. F. W., Protective Groups in Organic Chemistry (Plenum Press, London, 1973). Examples of suitable protecting groups for hydroxyl or mercapto substituents include substimted methyl ethers, for example, methoxymethyl, benzyloxymethyl, t-butyloxymethyl, 2-methoxyethoxymethyl, 1-ethoxyethyl, methylthiomethyl, 1-methyl- thioethyl, benzyl, allyl, triphenylmethyl and the like, other etherifying groups such as 2- tetrahydrofuryl, 2-tetrahydropyranyl and vinyl, or by acyl and carbonate groups such as formyl, 2,2-dichloroacetyl, 2,2,2-trichloroacetyl, t-butyloxy carbonyl, benzyloxycarbonyl, 4-nitrobenzyloxy carbonyl, and 4-methoxybenzyloxycarbonyl, or by silyl groups such as trimethylsilyl, t-butyldimethylsilyl, tribenzylsilyl, triphenylsilyl and the like. Suitable protecting groups for amino substituents include acyl groups such as formyl, acetyl, 3-phenylpropionyl, chloroacetyl, trifluoroacetyl, trichloroacetyl, benzoyl, 4-nitrobenzoyl, 4-methoxybenzoyl, t-butyloxycarbonyl, benzyloxycarbonyl, 4-nitrobenzyl- oxycarbonyl, 4-chlorobenzyloxycarbonyl, 4-methoxy benzyloxycarbonyl, 9- fluorenylmethoxycarbonyl, (2-pyridyl)methoxycarbonyl, quinoline-2-carbonyl, 2- trimethylsilylethoxycarbonyl, or trimethylsilyl, or an aminoacyl residue. Suitable protecting groups for carboxyl substituents include esters, for example methyl, ethyl, tert-butyl, benzyl, 4-nitrobenzyl, 4-methoxybenzyl, methoxymethyl, 2-methoxyethoxymethyl, benzyloxymethyl, methylthiomethyl, 2,2,2-trichloroethyl, 2- bromoethyl, 2-iodoethyl, 2-trimethylsilylethyl, 2-triphenylsilylethyl, t-butyldimethylsilyl or trimethylsilyl esters. Suitable protecting groups for carbonyl substituents include acetals such as dimethyl, diethyl, dibutyl and dibenzyl, thioacetals such as S,S-dimethyl and S,S-diethyl, cyclic acetals and thioacetlas such as 1,3-dioxanes, 1,3-dioxolanes, 1,3-oxathiolanes, 1,3-dithianes and 1,3-dithiolanes, and oximes and hydrazones such as O-benzyl oximes, O-phenylthiomethyl oximes and N,N-dimethyl hydrazones. The expression "solubilising group Px" as used herein refers to a group which may be used to derivatise a functional group so as to enhance the solubility of the compound of formula (I) in water or aqueous media. Examples of solubilising groups for inclusion in the compound of formula (I) are groups of the formula Px* or salts thereof, where Px* is selected from: X = O, S, S(O), S(O) 2 wherein R and R' are independently hydrogen or C -C 4 alkyl. Also included within the meaning of Px are groups of the following formulae, wherein Px* and D are as previously defined, and R is H or C -C 4 alkyl: Where the compound of formula (I) includes two functional groups capable of being derivatised by a solubilising group, the two funtional groups being in sufficiently close proximity to one another, it will be appreciated that certain of the solubilising groups exemplified above are capable of forming cyclic strucmres, for example including the following structural units: wherein Xi and X 2 are independently selected from O, S and NRg wherein Rg is as previously defined. Solubilising groups in a cyclic strucmre, such as those exemplifed above, also fall within the meaning of "solubilising group" as used herein. Where the solubilising group is acidic, a salt thereof is typically a salt of an alkali metal or ammonia, such as Na+, K+ or NH +. Where the solubilising group is basic, a salt thereof is typically a salt of a strong inorganic acid such as hydrochloric acid, sulfuric acid, phosphoric acid or nitric acid. Typically, the solubilising group is a sodium or potassium salt of a phosphate or phosphite residue. Solubilising or protecting groups which are included in the compound of formula (I) must be amenable to hydrolytic or metabolic cleavage in vivo. In one form of the present invention, in the compound of the general formula (I), B is typically selected from the group consisting of M 7 M 2 I I I ZM Mi M 2 D* — C— — c— — C— I I I II I I I — N — — N — — N— — C — , R14* R 14 R14 OR-I8 OR 15 — C— — C— I and I SR 19 NR 18 *R 19 * where Z, Z*, M, M 2 , D*, Rι , R i4 *, Rι ** , R 15 , R 18 , R 18* , R J9 and R i9 * are as previously defmed, and V is YR 2 , Y* or C(R 30 )=Y**, wherein R 2 , R 30 and Y** are as previously defined, and wherein Y is selected from the group consisting of N =N s ? " ? " -N-N-R 2 . — N=N— , — N= — , and Y* is selected from the group consisting of R R ,R33 — N-N=C — -0-R 2 . — 0-N-R 2 . R 50 " R " ' Rso and Rso ' wherein R 33> R34> R5O. R 51 and R 2* are as previously defined. More typically, the compound of the general formula (I) in this form of the invention has the strucmre represented by formula (IA): , where Ri * , Rι 0 , Rι 2 , Rι 2 *, R 13 and R !3* are as previously defined, B* is selected from the group consisting of M ZM M 2 I I I ZM Mi M 2 D * — C— — C— — C— — N i — — N ι — — N i — — C " — , Rι 4 * R14 I R14 where Z, Z*, M, Mj, M 2 , D*, Rι , R 14 *, R 14 **, Rι 8 and R 19 are as previously defined, and Yi is selected from the group consisting of -N— N-R 2 * — N-0-R 2 * -O— N-R 2 * I £ R50 R51 50 and R50 wherein R 50 , R 51 and R 2 * are as previously defmed. Even more typically, the compound of the general formula (I) in this form of the invention has the structure represented by formula (IB): wherein x and y are independently 0 or 1 , B is selected from the group consisting of wherein R 14 *, Rι 4 **, R 15 , Rι 8 and R 19 are as previously defmed and each R 5 g O is independently hydrogen or (C r C )alkyl, R 502 and R 506 are independently a group Rgoo, wherein Rgoo is selected from the group consisting of hydrogen, C(O)ORg 2 ι, C(O)SRg 2 ι, C(O)NRg 2 ιRg 22 , (C r C 6 )alkyl, (C 2 -C 6 )alkenyl, (C 5 -C 10 )cycloalkyl, (C 5 - Cιo)cycloalkyl(C r C 6 )alkyl, (C 5 -C 10 )cycloalkyl(C 2 -C 6 )alkenyl, (C 6 - Cιo)aryl, (C 6 -Cιo)aryl(C r C 6 )alkyl, (C 6 -Cι 0 )aryl(C 2 -C 6 )alkenyl, (C r C 6 )acyl, heterocyclic, heterocyclic(C r C 6 )alkyl and heterocyclic(C 2 - Cg)alkenyl, each of which may be substimted by up to three substituents selected from the substituents defined above for "optionally substimted (Cι-Cιg)alkyl" and R 2 ι and Rg 22 have the meaning of R 2J and R 22 respectively, as previously defined, or Rg 2 ι and Rg 22 together form a samrated or unsamrated cyclic, bicyclic or fused ring system as defined below, R 501 is selected from the group consisting of Rg 00 as previously defined, S(O)ORg 32 , S(O) 2 Rg 32 , S(O)NRg 32 Rg 33 , S(O) 2 Rg 32 Rg 33 , NH 2 , NHRg 31 and NRg 3i Rg 32 , wherein Rg 3i has the meaning of Rg as previously defined and Rg 32 and Rg 33 independently have the meaning of R 20 as previously defined, or R 501 and R 506 together form part of a samrated or unsamrated cyclic, bicyclic or fused ring system, or Rg 3 ι and Rg 32 , or Rg 32 and Rg 33 together form a samrated or unsaturated cyclic, bicyclic or fused ring system as defmed below, R512 and R5 4 2 independently have the meaning of R oo as previously defined, R522 anc * R532 are independently selected from the group consisting of Rgoo as previously defined, F, Cl, Br and I, R 5 l 3 and R5 43 are independently selected from the group consisting of Rgoo s previously defmed and R 2 QO as previously defined, R5 23 and Rs 33 are independently selected from the group consisting of R oo a s previously defined, F, Cl, Br, I, and R 00 as previously defined, R550 has the meamng of Rg as previously defined and R 55 ι is selected from the group consisting of Rg 50 , hydrogen, S(O)OR 32 , S(O) 2 Rg 32 , S(O)NRg 3 Rg 33 and S(O) 2 Rg 32 Rg 33 , wherein Rg 50 has the meaning of Rg as previously defmed and Rg 32 and Rg 33 are as previously defined, or Rg 32 and Rg 33 together form a samrated or unsamrated cyclic, bicyclic or fused ring system as defmed below, or R 55Q and one of R 55 and R 502 together form a diazaheterocycle wherein R550, R551 or R 502 and the two nitrogen atoms to which they are bonded are part of a stable 5 to 10- membered ring which may comprise up to two further heteroatoms selected from O, S and N and to which may be fused one or more cycloalkyl, cycloalkenyl, aryl or heterocyclic residues, which diazaheterocycle may be substimted by one or more of the substituents defmed above for "optionally substimted (C r Cιg)alkyl", and wherein two substituents may together form part of a ring, or one pair selected from R 5 ι 2 and R 5 ι 3 , R 522 and R 523 (when present), R 532 and R 533 (when present), and R 542 and R 543 , together are =O; O ^ R 15 wherein, when B is other than I or — C — then at least one of U I R14 * conditions (i) to (xi) below applies: (i) at least one of R 512 and R 542 is a group Rg 55 , wherein Rg 55 is selected from the group consisting of (C r C 6 )alkyl(C 6 -C 10 )aryl, (C 2 -C 6 )alkenyl- (Cg-Cιo)aryl, (C 5 -Cι 0 )cycloalkyl(C 2 -C 6 )alkenyl, (C 5 -Cι 0 )cycloalkyl- (C -Cιo)aryl, acyl(C 6 -Cι 0 )aryl, heterocyclic(C r C 6 )alkyl, hetero- cyclic(C 2 -C 6 )alkenyl, heterocyclic(C 6 -Cι 0 )aryl, C(D*)OR 2 ι*, C(D*)SR 21 * and C(D*)NR 2 ι*R 22 *, wherein D*, R 21 * and R 22 * are as previously defined, (ii) at least one of R 522 and Rs 32 , when present, is selected from the group consisting of Rg 55 as previously defmed, F, Cl, Br and I, (iii) at least one of R 5 ι 3 and Rs4 3 , when present, is selected from the group consisting of R 55 as previously defined, and R 0 o as previously defined, (iv) at least one of R 523 and R5 33 , when present, is selected from the group consisting of Rg 5 5 as previously defmed, F,C1 Br, I and R 0 o as previously defined, (v) R550 is a group Rg5g, wherein Rg 5 g is selected from the group consisting of (Cι-C 6 )alkyl(C 6 -Cιo)aryl, (C 2 -C 6 )alkenyl(C 6 -Cι 0 )aryl, (C 5 - Cι 0 )cycloalkyl(C 2 -C 6 )alkenyl, (C 5 -Cι 0 )cycloalkyl(C 6 -Cιo)aryl, acyl(C 6 - Cι 0 )aryl, heterocyclic(Cι-Cg)alkyl, heterocyclic(C 2 -Cg)alkenyl, hetero- cyclic(C 6 -Cιo)aryl, (vi) R551 is selected from the group consisting of Rg 56 as previously defined, S(O)ORg 32 , S(O) 2 Rg 32 , S(O)NRg 32 Rg 33 and S(O) 2 Rg 32 Rg 33 , wherein Rg 32 and Rg 33 are as previously defined, (vii) R502 is selected from the group consisting of Rg 5 g as previously defined, C(D*)SR 2 ι* and C(D*)NR 2 ι*R 22 *, wherein D*, R 2i * and R 22 * are as previously defined, (viii) R 502 and R551 are both hydrogen or are both (Cι-Cg)acyl, (ix) R J4 * is selected from the group consisting of C(D*)OR4 0 , C(D*)SR4 0 and C(D*)NR4 0 R4i, wherein R40 and R41 are as previously defmed, (x) R 5 oι is selected from the group consisting of Rg5 as previously defmed, S(O)ORg 32 , S(O) 2 Rg 32 , S(O)NRg 32 Rg 33 , S(O) 2 Rg 32 Rg 33 , NH 2 , NHRg 31 and NRg 3 ιRg 32 , wherein Rg 32 and Rg 33 are as previously defmed, (xi) R 50 ι and R 50 g are both (C r C 6 )acyl, OH and wherein when B is -C | - or ° 1 then at least one of the H — — following conditions also applies: (xii) x + y > 0, (xiii) x + y = 0 and at least one of R 532 and R 533 is other than hydrogen, (xiv) R50 and R51 together form a diazaheterocycle as previously defmed, (xv) at least one of R 50 ι, R502, R506 and R 551 is optionally substituted heterocyclic(Cι-Cι 8 )alkyl, and (xvi) at least one of R 5 ι 2 , R 542 , R 522 , R 532 , R 513 , R 543 , R 523 and R 533 is selected from the group consisting of C(O)ORg 21 , C(O)SRg 2 ι and C(O)NRg 2 ιRg 22 , wherein R 2 ι and Rg 22 are as previously defined. Examples of typical unsubstituted diazaheterocycles are: Other forms of the first embodiment of the invention have the strucmres represented by formulae (IC) to (IAW) below, in which each AA is independently a residue of a namrally occurring or synthetic amino acid as herein defined; R , Ri, X and X* are as previously defmed; Ra to Rj independently are -(CH 2 ) a . 6 OPy, wherein a can be 0, 1, 2, 3, 4 or 5, halogen or Rg, more typically -(CH 2 ) 0 . 3 OPy, fluoro, chloro or Rg* wherein Py is a solubilising group Px as defined herein, Rg is as previously defined and Rg* is is selected from the group consisting of hydrogen, R 20* , wherein R 2 Q* is selected from the group consisting of optionally substimted (Cι-Cg)alkyl, optionally substituted (C 2 -C 6 )alkenyl, optionally substimted (C 2 -C 6 )alkynyl, optionally substimted (C 3 -C 8 )cycloalkyl, optionally substimted (C 3 -C 8 )cycloalkyl(C r C 6 )alkyl, optionally substimted (C 3 -C 8 )cycloalkyl(C 2 -C 6 )alkenyl, optionally substimted (C 3 -C 8 )cycloalkyl(C 2 -C 6 )alkynyl, optionally substimted (C 6 -Cι 0 )aryl, optionally substimted (Cg-Cio)aryl(C r Cg)alkyl, optionally substimted (Cg-Cι 0 )aryl(C 2 -C 6 )alkenyl, optionally substituted (Cι-Cg)acyl, optionally substimted heterocyclic, and optionally substituted heterocyclic(Cι-Cg)alkyl, C(O)OR 2 ι, C(O)SR 2! , and C(O)NR 2 ιR 22 , wherein R 2i and R 22 independently are selected from hydrogen and R 20 * as previously defined, or R 2i and R 2 together form a samrated or unsaturated cyclic, bicyclic or fused ring system as previously defined: wherein D' is O or S, and each G is independently hydrogen or R 2Q O as previously defmed and wherein R'^ and R' f are R & and R f or, taken together, may be trimethylene or tetramethylene optimally substituted with -C(O)OR; or -C(O)NRiR j ; wherein G is selected from Ri* and X*Rι * ; wherein R a ' is OPy or Rg as previously defined, M is Rg as previously defined, (CH )ι_ 2 OPy or (CH 2 ) ! . 2 NHPy, and G* is OR 2 or NRjR 2 ; wherein G is hydrogen, R a , R X* or Rι * X*C(R a )(R b )C(O), and wherein R a , Ri*, and the atoms to which they are bound may optionally form a samrated or unsamrated cyclic, bicyclic or fused ring system; wherein R a , R , and the atoms to which they are bound may optionally form a saturated or unsamrated cyclic, bicyclic or fused ring system; (ID wherein W 2 is RiX or Rg as previously defined, and R' is Py or Rg as previously defmed, or R 1 and Py, taken together with the oxygen atoms to which they are attached form a HO p H O o o group selected from .A. , and ^ s & ^ -o o- -o o- -o o- wherein each L is independently as previously defined and each Pz is independently hydrogen or Py, provided that at least one Pz is Py or, when each Pz is Py, the groups Py, together with the oxygen atoms to which the are bound define a cyclic group selected wherein Q is O or NR f and G is R or X*Rι*; wherein each NHet) is independently a 5- or 6- membered samrated or unsamrated heterocycle containing a nitrogen atom and optionally additionally one or two heteroatoms selected from nitrogen, oxygen and sulfur, and wherein R a ' and R^' independently have the meaning of -(CH 2 )o_gOPy or Rg, or taken together are = O; (IM) wherein Wi is selected from RiX and Rι * X*, and Q is selected from O and NR h ; wherein W i is selected from RiX and Rι*X*, each Pz is independently hydrogen or Py, provided that at least one Pz is Py, and Q is selected from O and NR^; 5 wherein each Pz is independently hydrogen or Py, provided that at least one Pz is Py; wherein NHet) is a 5- or 6- membered samrated or unsamrated heterocycle containing a nitrogen atom and optionally additionally one or two heteroatoms selected from nitrogen, o oxygen and sulfur; wherein R a ' and R j ' are independently selected from Ri and R , as previously defined; Re Re Rα I I I 9 wherein G is selected from — C — ' — C— C — and a saturated or unsaturated I I I Rf Rf Rh cyclic, bicyclic or fused ring system, Q is O or NH, and G* is X or X* as previously defined; wherein NHet) is a 5-12 membered samrated or unsamrated cyclic, bicyclic or fused ring system containing a nitrogen atom and optionally additionally from 1 to 4 heteroatoms selected from nitrogen, oxygen and sulfur; (IT) wherein G is selected from hydrogen and Rι*X*, Q is O, S or NH, Q* is O or NH, and Gi is selected from Ri and Rι*X*; (IU) wherein R 2 oo is as previously defmed; wherein NHet) is an optionally substituted 5-12 membered samrated or unsamrated cyclic, bicyclic or fused ring system containing a nitrogen atom and optionally additionally from 1 to 4 heteroatoms selected from nitrogen, oxygen and sulfur; wherein b is 0, 1 or 2, provided that at least one b is greater than 0, and each Pz is independently hydrogen or Py, provided that at least one Pz is Py; wherein each G* is independently selected from O, S and NRg and G is selected from ORg, NHRg and R 20 ; wherein G is -C(O)- or -CH 2 -, G* is R 2 or Rj*, G** is -O- or -NR h -, Q is -O- or -NR j S o o ll li n II __-P-OH ϋ- ^ -OH / B-OH and Pz is selected from the group consisting of OH O 'H ° kff H ^O OH wherein R and R' are independently hydrogen or C 1 -C 4 alkyl, D is O or S and Px* is as previously defined; wherein G is Ri or Ri*, G* is -O- or -NR r and Pz is selected from the group consisting .Px* wherein R and R' are independently hydrogen or C r C 4 alkyl, D is O or S and Px* is as previously defined; wherein G is Ri or Ri * , and each Q is independently H, -OPz or -NP^Pz, wherein each P z is independently hydrogen or Py, provided that at least one Pz is Py; wherein N Het ) is a samrated or unsamrated cyclic, bicyclic or fused nitrogen containing ring system and G is a bond or is -O- or -NR ; wherein G is absent or X*Rι* and Het J is a 3 to 10-membered samrated or unsamrated heterocycle containing a nitrogen atom and optionally additionally one to three hetero¬ atoms selected from nitrogen, oxygen and sulfur; wherein Q is selected from -O-, -S- and -NR r ; OPy wherein G is O, S, S(O) or S(O) 2 , and R a ' and R b ' have the meamng of R a and R b or R a and R b - together are trimethylene or tetramethylene; wherein each Ar is independently (Cg-Cι 4 )aryl, R' c and R' d are R ς and R _ or, taken together, are -C(O)- or -CH(OH)-, and wherein Pz and Pz' are independently hydrogen or Py with the proviso that at least one of Pz and Pz' is Py, or Pz and Pz' together with the H0 ° H " p f 0 oxygen atoms to which they are attached form a group selected from ~ ° ° ~ , ~ ° ° ~ and -o o- OP, wherein G is a bond or X as previously defined, R g ' and R h ' are R g and R^ or together form a samrated or unsamrated cylic, bicylic or fused ring system, and Pz and Pz' are independently hydrogen or Py with the proviso that at least one of Pz and Pz' is Py, or Pz and Pz' together with the oxygen atoms to which they are attached form a group selected H % ° ° ° from -° / N o- -°' °- and ^ o- wherein G is a bond, O, S or NRj, R g ' and R h ' are R g and R h , or taken together may be - C(O)-, and Pz and Pz' are independently hydrogen or Py with the proviso that at least one of Pz and Pz' is Py, or Pz and Pz' together with the oxygen atoms to which they are HO. Jd H. / O O. / O attached form a group selected from ~ ° ° ~ , ~ ° 0_ and ~ ° 0_ ; OPy wherein G is OPy, NHRg, NPyRg or Rg; wherein G and G* are independently a bond, O, S or NH, and R' d and R h ' are Rd and R h or taken together are -CR' 2 - or -CR 2 '-CR 2 '- wherein each R * independently has the meaning of Rg as previously defined, Q and Q* are independently N or CRg, or when Q* is CRg then R g and Rg together may be a double bond; wherein G is -C(O)- or -C(R )(CH 2 ) 0 ^OG* wherein G* is Rg or Py; wherein G is selected from hydrogen and X*R and wherein C " J represents a 4-10 membered samrated or unsamrated cyclic, bicylic or fused ring system as defined herein; (IAN) wherein Q is selected from O, S and NR g , G and G* are independently selected from Ri, R l *, -C(R 5 )=NR 3 and -C(R 5 )=NOR 3 , wherein R 3 and R 5 are as previously defined, R' e and R' f are R g and R f , and G** is R 20 as previously defined; wherein each R z is independently selected from Ri and PyOG* wherein G* is optionally substimted alkylelne, provided that at least one R z is PyOG*, and G is -NR < ι- or CR d Rg-; ring system optionally containing up to three heteroatoms selected from N, O and S, G is selected from R XRi or X*Rι* and R a and R b taken together may optionally be -C(O)-; wherein B* is a group B, as previously defeined, derivatised with a solubilising group Py; wherein represents an optionally substimted cyclic, bicyclic or fused ring system containing a nitrogen atom and optionally additionally from 1 to 3 heteroatoms selected from N, O and S; wherein Qi and Q are independently selected from O and S, and R' f and R' g are respectively R f and R g or are selected from OR' , SR' and NR h R' wherein R' is H, R j or Py; wherein each G is independently selected from O and NR j , and R' is (CH 2 )ι_ 2 OPy or Rg; wherein G and G* are indep endently selected from and L, wherein L is as previously defined and Q is H or Py, provided that at least one of G and G* is other than L and provided that at least one Q is Py, or wherein two groups OQ taken together HO. JO H. JO / \ / \ are a cyclic group sleeted from , 0_ and -o Λ o- wherein R x and R y are independently Rg or (CH 2 )ι_ 2 OPy; wherein G and G* are independently selected from Ri, Ri*, -C(R 5 )=NR 3 and -C(R 5 )N=OR 3 , wherein R 3 and R 5 are as previously defined. Still other compounds of the first embodiment are those compounds exemplified in International Patent Application no. WO 93/18006, namely: (i) t-butyl 3-isopropyl-3-[(2R or S, 3S)-2-hydroxy-3-(phenylmethoxycarbonyl)- amino-4-phenylbuty 1] carbazate , (ii) t-butyl 3-isopropyl-3-[(2R or S, 3S)-2-hydroxy-3-(N-quinaldoyl-L-valyl)- amino-4-phenylbutyl] carbazate , (iii) t-butyl 3-isopropyl-3-[(2R or S, 3S)-2-hydroxy-3-(N-quinaldoyl-L- asparaginyl)amino-4-phenylbuty 1] carbazate , (iv) t-butyl 3-(l-methyl-3-phenylpropen-3-yl)-3-[(2R or S, 3S)-2-hydroxy-3- (phenylmethoxycarbonyl)amino-4-phenylbuty 1] carbazate , (v) t-butyl 3-(l-methyl-3-phenylpropyl)-3-[(2R or S, 3S)-2-hydroxy-3-(N- quinaldoy 1-L-asparaginy l)amino-4-phenylbutyl] carbazate , (vi) cis-l,6-3-t-butoxycarbonyl-4-[(2R or S, 3S)-2-hydroxy-3-amino-4-phenyl- buty 1] -3 , 4-diazabicy clo [4.4.0] decane , (vii) cis-l,6-3-t-butoxycarbonyl-4-[(2R or S, 3S)-2-hydroxy-3-(phenylmethoxy- carbony l)amino-4-phenylbuty 1] -diazabicyclo [4.4.0] decane , (viii) cis-l,6-3-t-butoxycarbonyl-4-[(2R or S, 3S)-2-hydroxy-3-(N-quinaldoyl-L- valyl)amino-4-phenylbutyl] -3 ,4-diazabicyclo [4.4.0] decane , (ix) cis-l,6-3-t-butoxycarbonyl-4-[(2R or S, 3S)-2-hydroxy-3-[N-(2-pyridyl)- methoxycarbony l)-L-valyl)amino-4-pheny lbutyl] -3 ,4-diaza-bicyclo [4.4.0]- decane, (x) cis-l,6-3-t-butoxycarbonyl-4-[(2R or S, 3S)-2-hydroxy-3-(N-quinaldoyl-L- asparaginy l)amino-4-pheny lbutyl] -3 ,4-diazabicyclo [4.4.0] decane , (xi) cis-l,6-3-t-butoxycarbonyl-4-[(2R or S, 3S)-2-hydroxy-3-(N-quinaldoyl-L- glutaminyl)amino-4-phenylbutyl]-3,4-diazabicyclo[4.4.0]decane, (xii) cis-l,6-3-t-butoxycarbonyl-4-[(2R or S, 3S)-2-hydroxy-3-(N-quinaldoyl-L- threonyl)amino-4-phenylbutyl]-3 ,4-diazabicyclo[4.4.0]decane, ____ (xiii) 2-t-butoxycarbonyl-3-[(2R or S, 3S)-2-hydroxy-3-(phenylmethoxycarbonyl)- amino-4-phenylbutyl]-2,3-diazabicyclo[2.2.1]nept-5-ene, (xiv) 2-t-butoxycarbonyl-3-[(2R or S, 3S)-2-hydroxy-3-(phenylmethoxycarbonyl)- amino-4-phenylbuty 1] -2 , 3 -diaza-bicyclo [2.2.1 ]heptane , (xv) 2-t-butoxycarbonyl-3-[(2R or S, 3S)-2-hydroxy-3-(N-(2-pyridyl)methoxy-L- valyl)amino-4-phenylbutyl]-2,3-diaza-bicyclo[2.2.1]heptane, (xvi) 2-[N-(lS)(2-methyl-l-methoxycarbonylpropyl)carbamoyl]-3-[(2R or S, 3S)-2- hydroxy-3-[N-(2-pyridyl)methoxy-L-valyl]amino-4-phenylbutyl]-2,3-diaza- bicyclo[2.2.1]heptane, (xvii) 2-t-butoxycarbonyl-3-[(2R or S, 3S)-2-hydroxy-3-(N-quinaldoyl-L- asparaginyl)amino-4-pheny lbutyl] -2 , 3-diazabicyclo [2.2.1 ]heptane , (xviii) l-[2-(2-pyridyl)methoxycarbonylamino-]benzoyl-2-[(2R or S, 3S)-2-hydroxy- 3-(N-quinaldoyl-L-asparaginyl)amino-4-phenylbutyl]-2-isopropyl-hydrazine, (xix) 2-t-butoxycarbonyl-3-[(2R or S, 3S)-2-hydroxy-3-(N-quinaldoyl-L- asparaginyl)amino-4-phenylbutyl]-l ,2,3 ,4-tetrahydrophthalazine, (xx) l-trimethylacetyl-2-[(2R or S, 3S)-2-hydroxy-3-(phenylmethoxycarbonyl)- amino-4-phyeny lbutyl] -2-isopropy lhy drazine , (xxi) l-trimethylacetyl-2-[(2R or S, 3S)-2-hydroxy-3-(N-quinaldoyl-L-asparaginyl) amino-4-pheny lbutyl] -2-isopropy lhy drazine , (xxii) l-(t-butylamino)carbonyl-2-[(2R or S, 3S)-2-hydroxy-3-(N-quinaldoyl-L- asparaginyl)amino-4-pheny lbutyl] -2-isopropy lhy drazine , (xxiii) t-butyl 3-isopropyl-3-[(2R or S, 3S)-2-hydroxy-3-(N-picolinoyl-L- asparaginyl)amino-4-pheny lbutyl] carbazate , (xxiv) t-butyl 3-isopropyl-3-[(2R or S, 3S)-2-hydroxy-3-(N-(2-pyridyl)-methoxy- carbonylanthraniloyl)amino-4-pheny lbutyl] carbazate . (xxv) t-butyl 3-benzyl-3-[(2R or S, 3S)-2-hydroxy-3-(phenylmethoxycarbonyl)- amino-4-pheny lbutyl] carbazate , (xxvi) t-butyl 3-benzyl-3-[(2R or S, 3S)-2-hydroxy-3-(N-quinaldoyl-L-asparaginyl)- amino-4-pheny lbutyl] carbazate, (xxvii) t-butyl 3-cyclohexyl-3-[(2R or S, 3S)-2-hydroxy-3-(phenyl-methoxy- carbony l)amino-4-pheny lbutyl] carbazate , (xxviii) t-butyl 3-cyclohexyl-3-[(2R or S, 3S)-2-hydroxy-3-(N-quinaldoyl-L- asparaginy l)amino-4-pheny lbutyl] carbazate , (xxix) t-butyl 3-isopropyl-3-[(2R or S, 3S)-2-hydroxy-3-(N-(l-carbamoyl-methyl)- acryloyl)amino-4-phenylbutyl]carbazate, (xxx) t-butyl 3-isopropyl-3-[(2R or S, 3S)-2-hydroxy-3-(N-(2(RS)-3-tert-butylthio- 2-carbamoyl-methy lpropiony l)amino-4-pheny lbutyl] carbazate , (xxxi) t-butyl 3-isopropyl-3-[(2R or S, 3S)-2-hydroxy-3-(N-(l-benzoyl-L- asparaginy l)amino-4-pheny lbutyl] carbazate , (xxxii) l-t-butyloxycarbonyl-2-[(2R or S, 3S)-2-hydroxy-3-(phenylmethoxy- carbonyl)amino-4-phenylbutyl]hexahydropyridazine, (xxxiii) l-t-butyloxycarbonyl-2-[(2R or S, 3S)-2-hydroxy-3-(N-quinaldoyl-L- asparaginyl)amino-4-phenylbutyl]hexahydropyridazine , and (xxxiv) cis-l,6-3-t-butoxycarbonyl-4-[(2R or S, 3S)-2-hydroxy-3-(N-quinaldoyl- 3-cyano-L-alanyl)amino-4-phenylbutyl]-3,4-diaza-bicyclo[4,4,0]decane, wherein the 2-hydroxy group has been derivatised with a solubilising group Px as herein defined. Typically, in this form of the first embodiment, compounds (i) to (xxxiv) o II referred to above are derivatised with a solubilising group selected from / p v 0H and o II / -OH . H The compounds of formulae (I) to (LAW) can exist in optically isomeric forms and the present invention includes within its scope all these forms in all proportions including all diastereoisomers and mixtures thereof and all enantiomers, mixtures of enantiomers and racemic mixtures. Where a double bond occurs in the compound of the invention, the double bond may be present in the cis- (Z) or trans- (E) configuration. It will be understood that only compounds of formula (I) with combinations of substituents or functional groups which give rise to stable compounds, are within the scope of the present invention. The compounds of general formula (I) may be prepared by methods known generally in the art. Suitable methods for the synthesis of compounds of formula (I) and intermediates thereof are described, for example, in Houben-Weyl, Methoden der Organischen Chemie; J. March, Advanced Organic Chemistry, 3rd Edition (John Wiley & Sons, New York, 1985); D. C. Liotta and M. Volmer, eds, Organic Syntheses Reaction Guide (John Wiley & Sons, Inc., New York, 1991); R. C. Larock, Comprehensive Organic Transformations (VCH, New York, 1989), H. O. House, Modern Synthetic Reactions 2nd Edition (W. A. Benjamin, Inc., Menlo Park, 1972); N. S. Simpkins, ed. 100 Modern Reagents (The Royal Society of Chemistry, London, 1989); A. H. Haines Methods for the Oxidation of Organic Compounds (Academic Press, London, 1988) and B. J. Wakefield Organolithium Methods (Academic Press, London, 1988). For example, a compound of formula (I) may be prepared from synthons W*, {(A) n -B-(A*) m }* and V*, wherein each synthon identified thus * is a synthetic precursor of the corresponding portion of the molecule W-(A) n -B-(A*) m -V. Thus, a compound of formula (I) may be prepared, for example, in any of the following ways: (a) by reaction of W-(A) n -B-(A) m -G with H-V; (b) by reaction of W-(A) n -B-(A) m -H with G-V; (c) by reaction of W-H with G-(A) n -B-(A) m -V; and (d) by reaction of W-G with H-(A) n -B-(A) m -V; wherein G is a leaving group such as halogen, typically chlorine, bromine or iodine; a sulfonate such as methanesulfonate, trifluoromethanesulfonate, benzenesulfonate or toluenesulfonate; an alkoxy, thioalkoxy, aryloxy or thioaryloxy group such as ethoxy, methoxy, thiomethoxy or phenoxy; acyloxy such as acetyl, trifluoroacetyl or benzoyl; hydroxy; amino or protonated amino; nitrate; phosphate; borate and the like. If appropriate these reactions may be carried out in the presence of a base such as triethylamine, pyridine or other tertiary amine, butyllithium, sodium tert-butoxide or similar, and/or a coupling reagent such as a carbodiimide. When V is YR 2 where Y is — N=N — , or when V is Y* where Y* is a member of the group — N— N-R 2 * — N-0-R 2 * — O— N-R 2 * I I £ I I 2 R50 R5I R 50 and 50 the compound of formula (I) may be prepared as shown in Scheme 1 or Scheme la. In the Schemes and in the Examples herein, the terms Me, Et. Pr, Ph and Bz signify methyl, ethyl, propyl, phenyl and benzyl respectively and the following additional abbreviations are used: THP tetrahydropyranyl, t-Bu or Bu l tertiary butyl n-Bu n-butyl iPr or Pr isopropyl Hal halogen; i.e. , fluorine, chlorine, bromine or iodine Ts para-toluenesulfonyl DMF dimethyl formamide CDI N,N'-carbonyldiimidazole BOP benzotriazol-l-yloxytris(dimethylamino)-phosphonium hexafluoro- phosphate HBT 1-hydroxybenzotriazole AcCN acetonitrile DMSO dimethyl sulfoxide Py.xSO 3 pyridine/sulfur trioxide complex QC quinoline-2-carbonyl PC 2-pyridinemethoxycarbonyl MC N-morpholinocarbonyl TMC N-thiomorpholinocarbonyl Val valinyl Asn asparaginyl He isoleucyl Gly glycinyl Glu glutaminyl Thr threonyl Ala alanyl W-(A) n -B-(A* -tl-R 2 H H Oxidation W-(A) n -B-(A*)rtτN=N-R 2 Other compounds of formula (I) may be prepared analogously, by reacting a synthon W-(A) n -B-(A*) m -Hal with HV, if appropriate in the presence of a strong base. Scheme 1a (RO) 2 C(0) R a NHNH 2 R a NHNHC(0)OR base RbHal base H 3 0 Ra— N— NH 2 Ra— N— NHC(0)OR Rb Rb RcHal base Ra— N— NHRc Rb In Scheme la, R represents an alkyl, aryl or aralkyl group, such as t-butyl, phenyl or benzyl. Suitable bases include pyridine, triethylamine and other tertiary amines, alkali metal carbonates and alkali metal hydroxides. The moiety W-(A) n -B-(A*) m - may be represented by R a , in which case R b represents R 50 as previously defined, and R ς represents R 2 as previously defmed, or W-(A) n -B-(A*) m - may be represented by Rr_, in which case R 5 represents R 51 and R a represents R 2 . When V is Y* where Y* is — N-N=C N , the compound of formula (I) may be R50 prepared from by reacting a hydrazine wherein R 5l and R 2 * are both hydrogen, which may be prepared as shown in Scheme 1 or Scheme la, with an aldehyde or ketone. o- o- When V is YR 2 where Y is _ N=r ! j _ or __^ =N _ , the compound of formula + + (I) may be prepared as shown in Scheme lb Scheme 1 b W-(A)n-B-(A*)m-Hal + R 2 -N=N-0 " W-(A) ιr B-(A * ) rπ N=N-R 2 O W-(A)n-B-(A*)m-N=N-0- R 2 -Hal W-(A) n -B-(A * )m N=N-R 2 O When V is YR 2 where Y is a member of the group o o o o o II II II II II — S-N— — S-N— — N-S— — N-S— — O-S — I II I I I II H R50 O R50 R50 R50O o p 0 0 o o II II -s -s— -o-s- — s-o- I -o— -s I II — s II— s- o o o o o 0 0 II II II II — S— S— — P— N — — 0-P— N— — N-P— — N— P-O— I I I I I I I I R 5 10 R50 R510 R50 R50OR 5 1 R 5 0OR 5 1 0 0 0 0 0 II II II II II — P— 0— — 0— P — — P— N — — N— P — — P— O— I I I I I I I OR 51 OR 51 R 51 O R 50 R5QOR 51 R 52 the compound of formula (I) may be synthesised by coupling a synthon W-(A) n -B-(A*) m - Z a with a synthon Zt,, where Z a includes one of the heteroatoms of Y, and Z b includes the other heteroatom or atoms, as shown in schemes 2a and 2b: Scheme 2a O W-(A),rB-(A*)mO-H CIS(0)R;_ - W-(A) ιr B-(A * ) rπ O-S-R 2 HSR, W-(A) rr B-(A * ) r T S-H W-(A) ιr B-(A * ) rτr S-S-R 2 Scheme 2b O II O HNR 50 R 2 II W-(A)n-B-(A * )ffl-S-CI W-(A) ιr B-(A * ) m -S-N-R 2 R50 O HNR50R2 o W-(A) n -B-(A * ) m -έ-CI W-(A)π-B- (A^m-S-N-Rz O O R50 W-(A) π -B-(A*) ήr O O HOR ? II W-(A) n -B-(A*) ffr S-CI W-(A) n -B-(A*) r r S-0-R 2 O HOR, O W-(A) n -B-(A*) -P-CI W-(A) n -B -(A * )ήrP-0-R 2 OR 51 OR51 O II HO R, O W-(A) tr B-(A*) tπ -0-P-CI W-(A) r B-(A * ) rπ -0-P-0-R 2 OR 51 OR51 Analogous methods may be used to obtain the corresponding thionophosphates and thionophosphonates. When V is C(R 3 Q)=Y** the compound of formula (I) may be prepared from a synthon having a ketone or aldehyde function, by condensation with a substimted hy drazine or substimted hydroxylamine corresponding to Y**. When V is Y*, where Y* is -N=O, the compound of formula (I) may be prepared by oxidising the corresponding primary amine, for example with Caro's acid, or H 2 O 2 in acetic acid, or H O with sodium tungstate. It will be appreciated that a compound of formula (I) wherein Y* is -N=O will only be isolable as a nitroso compound when the carbon atom bearing Y* has no α-hydrogens. 0 — S=0 =0 When V is Y* where Y* is l_ or I , the compound of formula R 114* R-114* (I) may be prepared by oxidation of the corresponding thioether W-(A) n -B-(A*) m -S-Rn 4 * (IV) with hydrogen peroxide and acetic acid. The thioether (TV) may be synthesised by coupling a halide W-(A) n -B-(A*) m -Hal with a thiol R 114 * under basic conditions, or by reacting a disulfide Rn 4 *SSRιi 4 * with an organolithium reagent W-(A) n -B-(A*) m -Li derived from the corresponding halide. OR 115 R-114* I — P =0 -P=0 When V is Y*, where Y* is 1 I or I R-I-I4 the compound of formula R114** (I) may be prepared by the Arbuzov reaction as shown in scheme 3: Scheme 3 R 114 * MeO-P I R-114** R114* W-(A) π -B-(A * ) r r Hal W-(A) ιr B-(A * ) rτr P=0 R114* The synthon W-(A) n -B-(A*) m -Z, where Z is any of the functional groups bound to (A*) m which are represented in schemes 1 to 3, may be prepared by coupling a suitably fiinctionalised fragment W* with a correspondingly fiinctionalised fragment Z*-(A) n -B- (A*) m -Z. Alternatively, the compound of formula (I) may be synthesised by first coupling V to (A) n -B-(A*) m - as described above with reference to schemes 1 to 3, and then coupling the resulting molecule to a fiinctionalised fragment W*. Methods for coupling a precursor of group W with a fiinctionalised fragment Z*-(A) n -B-(A*) m -Z are well known in the art, and include methods analogous to those represented in schemes 1 to 3. For example, when W is RiX and X is Y, the coupling may be achieved as described in schemes 1 to 3 above. When W is R X and X is NRι 0 , O or S, the coupling may be achieved by any of the known methods for the alkylation of amines, and the synthesis of ethers and thioethers, respectively. That is, the coupling may be achieved by reacting a fragment Z*-(A) n -B-(A*) m -Z wherein Z* is a leaving group such as halogen, sulfonate ester, acetate or frialkylammonium salt, with RIRI Q NH, RiOH or RiSH, if necessary in the presence of strong non-nucleophilic base such as butyllithium, sodamide or potassium tert-butoxide. Compounds in which X is S(O) or S(O) 2 may be prepared by the oxidation of the corresponding compound in which X is S. Compounds in which W is -CN, -C(R 5 )=NR 3 , -C(R 5 )=NOR 3 , -C(D)OR 3 , -C(D)SR 3 or -C(D)NR 3 R 4 may be prepared from the fragment Z*-(A) n -B-(A*) m -Z wherein Z* is an aldehyde, ketone or carboxyl group as shown in Scheme 3a. Scheme 3a Compounds in which W is -N=CR 5 R 5* may be prepared by reacting the fragment Z*-(A) n -B-(A*) m -Z, where Z* is NH 2 , with an aldehyde or ketone having group(s) R 5 and R 5 * bound to the carbonyl. The fragment Z*-(A) n -B-(A*) m -Z may be prepared by methods which depend on the nature of B. Where B is a substimted carbon atom, the fragment may be conveniently prepared from a fragment E-C(O)-E*, in which E is a fragment Z*-(A) n and E* is a fragment (A*) m -Z, as shown in scheme 4: Scheme 4 CH 2 OH E-C-E* Rι 4 O Fragments which are starting materials for compounds of formula E-C-E* (I) are known compounds or analogs of known compounds which can be prepared by methods analogous to methods used for preparation of the known compounds. The O synthesis of known fragments || may be found with reference, for example, to E-C-E* Beilsteins Handbuch der Organischen Chemie or to J. Buckingham, ed., Dictionary of Organic Compounds 5th Edition (Chapman & Hall, New York, 1982). Alternatively, a fiinctionalised group E may be coupled to a group E*C(O)H, or a fiinctionalised group E* may be coupled to a group EC(O)H, followed by oxidation. For example, a halide EBr may be coupled to E*C(O)H with an organolithium or organomagnesium reagent derived from EBr, followed by oxidation of the resulting secondary alcohol to the corresponding ketone, if desired. Alternatively a carboxylic acid EC(O)OH may be converted to an activated derivative, such as an ester or amide: for example an amide obtained by reaction of the carboxylic acid with N,O-dimethyl hydroxy lamine hydrochloride in the presence of a carbodiimide and tertiary base, followed by addition of an organolithium or organomagnesium reagent derived from E*Br, E*C1 or E*I. O / \ When B is an epoxide of the type V V the fragment E-B-E* may be Rl4*Rl4** prepared from the corresponding olefin by reaction with a per-acid such as trifluoroper- acetic acid, perbenzoic acid or m-chloroperbenzoic acid. Suitable olefins for conversion to the fragment E-B-E* are commercially available or may be synthesised by known methods, for example by means of the Wittig reaction or by an elimination reaction of an alcohol, alcohol sulfonate, ester, halide or the like. When B is a diol of the type , the compound of formula (I) may conveniently be prepared by reductive coupling of aldehydes EC(O)H and E*C(O)H as described in J. Org. Chem 55, 4506 (1990) and U.S. Patent No. 5,294,720. When B is a heteroatom or substimted heteroatom, the fragment Z*-(A) n -B- (A*) m -Z is a substimted amine, phosphine or phosphine oxide, or is an ether, thioether, sulfoxide or sulfone. Substimted amines, ethers, thioethers, sulf oxides and sulfones may be prepared as described above. Secondary or tertiary phosphines may be prepared by alkylation of the corresponding primary or secondary phosphine as described, for example, in J. D. Roberts and M. C. Caserio, Basic Principles of Organic Chemistry (W.A.Benjamin, Inc., New York, 1965). In any of the reactions described above, it may be necessary to protect reactive group(s) in the compound of formula (I) other than those participating in a desired coupling or oxidation reaction using suitable protecting group(s) in order to carry out the desired coupling or oxidation reaction without chemically affecting those reactive groups. Suitable protecting groups for this purpose are described in the works of Greene and McOmie referenced above. The compounds of formula (IB) wherein x and y are both 1 may be prepared as generally described above. A compound of formula (IB) which is where R a and R, have the meaning of R 501 and R 506 as previously defined and R,, and R _ have the meaning of R 551 and R 5 Q 2 as previously defined, may be prepared from ethylene cyanohydrin by the method shown in Scheme 5. Scheme 5 ZnBιyCH 2 CI 2 A substituted compound of formula (IB) may be prepared by the general method of Scheme 5, with the substiments R 5 ι 2 , R 5 ι 3 , R 522 , R 523 , R 532 , R 533 , R 542 , R 543 and R 550 being introduced, as desired, into the compounds of formula (Va), (Vb), (Vc) and (Vd) shown in Scheme 5 by the methods illustrated in Scheme 5a. Scheme 5a OCH 2 0(CH 2 ) 2 OCH 3 H OCH 2 0(CH 2 ) 2 OCH 3 TsCI, Me^O (Vc) HO' ^ OBz O^^^^OBz RMgHal 5a-4 R R' OCH 2 0(CH 2 ) 2 OCH 3 R OCH 2 0(CH 2 ) 2 OCH 3 1. Me 2 CO, AI(OBut) 3 ^ OBz >Bz 2. R'MgHal 5a-5 H 2 ) 2 OCH 3 In reaction 5a-l shown above, it will be appreciated that the step of introducing the second substituent R' will only be carried out if it is desired that both R 52 and R 523 be other than hydrogen. The reactions shown in 5a-2 and 5a-3 may be repeated, if desired, so as to introduce a second substituent on the carbon atom bearing R" or R"C(O). The second substituent can be the same as or different from the first. Where one or both of Rs 22 and R 523 is acyl, this group may be introduced as shown in reaction 5a-3 with respect to compound (Vb). Where R 52 and R 523 are both hydrogen, the reactions shown in 5a-2 and 5a-3 may give mixmres of products and in that case it may be preferable to introduce the desired groups Rs 3 , R 543 , R 542 and R 543 by replacing the ethylene bromohydrin shown in Scheme 5 with a suitably substimted bromohydrin obtained from the corresponding olefin as shown in Scheme 5b. It will be appreciated that the nature of the groups Rs 32 , Rs4 3 , Rs4 and R 5 3 will determine the stereochemistry of the addition of HOBr to the olefin and of the opening of the epoxide. Scheme 5b Compounds of formula (IB) wherein B is other than -CH(OH)- may be prepared by the methods shown in Scheme 4 after oxidation of the secondary alcohol to the corresponding ketone. The compounds of formula (IB) wherein B is a substimted carbon atom and y is 0 can be prepared by reacting a compound of formula (II), (II A) or (LIB) (ii) (HA) (HB) wherein R 14 *. R 50 ι, R502. R5O6' R 512» R 513' R 522> 523 ' R 542. and R543 have the significance given earlier and Hal is a group selected from -Cl, -Br or -I, with a compound of formula (III) wherein R 50 , R 550 and R 55 j have the significance given earlier. Where a compound of formula (II) is used, the reaction may be followed by oxidation of the resultant secondary alcohol to the corresponding ketone. This ketone may be used for elaboration of the substituents on B as shown in Scheme 4. A compound of formula (II), (II A) or (TIB) may be prepared from a β-amino acid or a β-amido acid as shown in Scheme 6. A compound of formula El may be prepared as shown in Scheme la. Scheme 6 1. Li, MeNH 2 2. H 3 0 + An alternative route to the β-aminoaldehyde shown in Scheme 6 is by reduction of the methyl ester of the corresponding β-amino acids using diisobutylaluminium hydride. β-amino acids, or β-amido acids, may conveniently be prepared by the Mannich reaction of an amine or amide with an enolisable ketone in the presence of formaldehyde or another aldehyde. A compound of formula (IB) wherein x and y are both 0 may be prepared by reacting a compound of formula (EC) or (IID) (IIC) (IID) with a compound of formula (IE) as shown above. An analogous procedure, utilising a primary or secondary amine rather than a hydrazine as shown in formula (ϋl) yields a hydroxy diamine. A compound of formula (EC) may be prepared from an α-amino acid by a method analogous to that shown in Scheme 6, such as described in the following: Evans, B.E., et al., J. Org. Chem. , 50, 4615-4625 (1985); Luly, J.R., et al., J. Org. Chem. , 52, 1487-1492 (1987); Handa, B.K., et al., European Patent Application No. 346,847-A2 (1989) and Marshall, G.R., et al., International Patent Application No WO91/08221. Suitable α-amino acids may be prepared, for example, by the Strecker synthesis, starting from an appropriate ketone. The overall route to the compound of formula (IIC) is shown in Scheme 7. Other suitable methods are described in Coppola, et al. Asymmetric Synthesis. Construction of Chiral Molecules using Amino Acids (Wiley Interscience, New York, 1987). Scheme 7 R, 512 RC(0)CI Where W is a nitrogen-containing group, and one of Ri and R J0 is a protected amino acid residue, the coupling of the protected amino acid residue may be accomplished as shown in Scheme 8, in which the amino acid (designated AA) protecting group is benzyloxycarbonyl, designated Z. Methods for the formation of peptide bonds and for the protection of peptide residues are described, for example, in Gross and Meienhofer, eds. , The Peptides, (Academic Press, New York, 1983). Suitable other coupling agents include l-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride (EDC) and diphenyl- phosphoryl azide (DPP A). Scheme S BOP, HBT, EtNfl-Pr DMF, HN(R)-(A)-B-(A*)-V o Z ^AA- N(R)"(A)"B"(A*)_V Numerous synthetic routes exist to substimted hydrazines, including the hydrazines of formula (El), useful in the synthesis of compounds of formula (I). The hydrazine intermediates (III) can be obtained using known methods such as those described in the following: Dutta, A.S., et al., J. Chem. Soc. Perkin Trans. I, (1975) 1712-1720, Ghali, N.I., et al., J. Org. Chem. , 46, 5413-5414 (1981), Gante, J., Synthesis (1989) 405-413 and Houben-Weyl's Methoden der Organische Chemie, vol. 16a, Part 1, pp 421-855; Georg Thieme Verlag, Stuttgart (1990) Other methods for preparing substimted hydrazines are illustrated in Scheme 9. Scheme 9 (x= 1 or2) * " NH 2 R= N -OH Compounds of formula (I) wherein a group selected from R^ Ri * , R 2 , R 2* , R 9 , Rn, R 2 , R 50 and R 5i , together with another group selected from Ri, Ri * , R 2 , R 2* , R 9* , Rio, Rn, Rι 2 , R 50 and R 5J forms a cyclic, bicyclic or fused ring system may be prepared by variants on the above methods which will be readily apparent to persons skilled in the art in the light of the foregoing. An example of a method of preparing one class of cyclic compounds of formula (I) is presented in Scheme 10: Scheme 10 Compounds in accordance with the present invention which do not include a solubilising group Px typically exhibit low to very low water solubility. Inhibitors of HIV proteases which have hitherto been described, and many other pharmaceutically or veterinarily active substances also typically exhibit low to very low water solubility. This property tends to cause the bioavailability of such substances to be relatively low. There is thus a need for a HIV protease inhibitor having enhanced water solubility. Surprisingly, it has been found that the inclusion of a solubilising group Px as defined herein in a substance having low to very low water solubility results in enhancement of the water solubility of the substance. Thus, substances in accordance with the invention which include a solubilising group Px exhibit superior bioavailability, including superior oral bioavailability, compared to compounds in accordance with the invention which do not include a solubilising group Px. Thus, according to a second embodiment of the present invention, there is provided process for enhancing the water-solubility of a pharmaceutical or veterinary substance, comprising derivatising a functional group of said substance with a solubilising group Px, wherein Px is selected from the group consisting of Px*, or S, R is H or C 1 -C 4 alkyl, and wherein said functional group being capable of being derivatised with said solubilising group Px. Generally, a compound according to the first embodiment includes at least one solubilising group Px as defined above. More generally, a solubilising group in a o compound of the first embodiment or in the method of the second embodiment is selected o o from _. -P-OH and .P-OH OH H Typically, a solubilising group is introduced into the molecule as the last stage of its synthesis. For example, a solubilising group P(O)(OH) 2 may be introduced to a free amino, hydroxy or mercapto group by reaction of the amino, hydroxy or mercapto group 5 with dimethyl chlorophosphate, followed by mild hydrolysis to remove the methyl ester groups. Other solubilising groups referred to above may be introduced by analogous methods: that is, by reaction of an amino, hydroxy, mercapto or other group capable of being derivatised with a solubilising group, with a reagent PxX' , suitably protected if necessary (for example as methyl or benzyl esters), wherein Px is as defined above and X' 0 is a leaving group such as Cl, Br, OH, OS(O) 2 R and the like, where R is C r C 6 alkyl, for example methyl, C 6 -Cι 0 aryl, for example phenyl or 4-methylphenyl, or C 7 -Cn arylalkyl, for example benzyl. Alternatively, a solubilising group P(O)(OH) 2 may be introduced to a free hydroxy group by reaction with phosphorous acid and mercuric salts in the presence of a tertiary amine, as described by Obata and Mukaiyama in J. Org. Chem. , 32, 1063 (1967). As a further alternative, an amino, hydroxyl or mercapto group may be reacted with phosphorous acid preferably in the presence of a coupling agent such as dicyclohexylcarbodiimide and pyridine to yield a molecule possessing the solubilising group -OP(O)(OH)H. Optionally, this group may be oxidised to the corresponding phosphate derivative, for example using bis(trimethylsilyl) peroxide (see Scheme 14 below for an illustration of this method). A further process for the introduction of a group -P(O)(OH) 2 is described in Australian patent application no. 54311/86, and involves the reaction of an amino, hydroxy or mercapto group with certain diesters of amides of phosphorus acid, followed by oxidation and hydrolysis of the resulting intermediate compounds. Suitable reagents for the introduction of a solubilising group -NO 2 are lower alkyl nitrates such as methyl mtrate or ethyl nitrate, and acyl nitrates such as acetyl nitrate or benzoyl nitrate. Other methods for the preparation of compounds of formulae (I) to (IAW) referred to herein are disclosed in US Patent Nos. 5,116,835, 5,126,326; 5,132,400; 5,145,957; 5,198,426; 5,212,157; 5,215,968; 5,212,667; 5,294,720; and 5,296,604; International Patent Application Nos. 91/08221; 91/10442; 92/151319 and 92/21696; European Patent Application Nos. 0528242; 0519433 and 0432595 and Australian Patent Application Nos. 35700/89; 53716/90; 63221/90; 71319/91; 71320/91; 71323/91; 82313/91; 83206/91; 87594/91; 90531/91; 90851/94; 90925/91; 91251/91; 91332/91; 18355/92; 26424/92; 37160/93; 38808/93 and 44930/93, the disclosures of each of which are incorporated herein by reference. A third embodiment of the invention is directed to pharmaceutical compositions comprising a compound of formula (I) together with one or more pharmaceutically acceptable carriers, diluents, adjuvants and/or excipients. In a fourth embodiment of the invention there is provided a method for inhibiting retroviral proteases in a mammal in need of such inhibition, comprising administering to the mammal an effective amount of a compound of the first embodiment or of a composition of the second embodiment. In one form of the third embodiment, there is provided a method for the treatment or prophylaxis of HIV viral infections such as AIDS. For inhibiting retroviral proteases or the treatment of HIV viral infections, a composition of the second embodiment may be administered orally, topically, parenterally, e.g. by injection and by intra-arterial infusion, rectally or by inhalation spray. For oral administration, the pharmaceutical composition may be in the form of tablets, lozenges, pills, troches, capsules, elixirs, powders, including lyophilised powders, solutions, granules, suspensions, emulsions, syrups and tinctures. Slow-release, or delay ed-release, forms may also be prepared, for example in the form of coated particles, multi-layer tablets or microgranules. Solid forms for oral administration may contain pharmaceutically acceptable binders, sweeteners, disintegrating agents, diluents, flavourings, coating agents, preservatives, lubricants and/or time delay agents. Suitable binders include gum acacia, gelatin, corn starch, gum tragacanth, sodium alginate, carboxymethylcellulose or polyethylene glycol. Suitable sweeteners include sucrose, lactose, glucose, aspartame or saccharine. Suitable disintegrating agents include corn starch, methylcellulose, polyvinylpyrrolidone, xanthan gum, bentonite, alginic acid or agar. Suitable diluents include lactose, sorbitol, mannitol, dextrose, kaolin, cellulose, calcium carbonate, calcium silicate or dicalcium phosphate. Suitable flavouring agents include peppermint oil, oil of wintergreen, cherry, orange or raspberry flavouring. Suitable coating agents include polymers or copolymers of acrylic acid and/or methacrylic acid and/or their esters, waxes, fatty alcohols, zein, shellac or gluten. Suitable preservatives include sodium benzoate, vitamin E, alpha-tocopherol, ascorbic acid, methyl paraben, propyl paraben or sodium bisulphite. Suitable lubricants include magnesium stearate, stearic acid, sodium oleate, sodium chloride or talc. Suitable time delay agents include glyceryl monostearate or glyceryl distearate. Liquid forms for oral administration may contain, in addition to the above agents, a liquid carrier. Suitable liquid carriers include water, oils such as olive oil, peanut oil, sesame oil, sunflower oil, safflower oil, arachis oil, coconut oil, liquid paraffin, ethylene glycol, propylene glycol, polyethylene glycol, ethanol, propanol, isopropanol, glycerol, fatty alcohols, triglycerides or mixmres thereof. Suspensions for oral administration may further comprise dispersing agents and/or suspending agents. Suitable suspending agents include sodium carboxymethylcellulose, methylcellulose, hydroxypropylmethylcellulose, polyvinyl¬ pyrrolidone, sodium alginate or cetyl alcohol. Suitable dispersing agents include lecithin, polyoxyethylene esters of fatty acids such as stearic acid, polyoxyethylene sorbitol mono- or di-oleate, -stearate or -laurate, polyoxyethylene sorbitan mono- or di-oleate, -stearate or -laurate and the like. The emulsions for oral administration may further comprise one or more emulsifying agents. Suitable emulsifying agents include dispersing agents as exemplified above or natural gums such as gum acacia or gum tragacanth. For topical administration, the pharmaceutical composition may be in the form of a cream, ointment, gel, jelly, tincture, suspension or emulsion. The pharmaceutical composition may contain pharmaceutically acceptable binders, diluents, disintegrating agents, preservatives, lubricants, dispersing agents, suspending agents and/or emulsifying agents as exemplified above. For parenteral administration, the compound of formula I or its salt may be prepared in sterile aqueous or oleaginous solution or suspension. Suitable non-toxic parenterally acceptable diluents or solvents include water, Ringer's solution, isotonic salt solution, 5% dextrose in water, buffered sodium or ammonium acetate solution, 1,3- butanediol, ethanol, propylene glycol or polyethylene glycols in mixtures with water. Aqueous solutions or suspensions may further comprise one or more buffering agents. Suitable buffering agents include sodium acetate, sodium citrate, sodium borate or sodium tartrate, for example. Aqueous solutions for parenteral administration are also suitable for administration orally or by inhalation. For rectal administration, the compound of formula I is suitably administered in the form of an enema or suppository. A suitable suppository may be prepared by mixing the active substance with a non-irritating excipient which is solid at ordinary temperatures but which will melt in the rectum. Suitable such materials are cocoa butter, waxes, fats, glycerol, gelatin and polyethylene glycols. Suitable enemas may comprise agents as exemplified above with reference to forms for topical administration. Suitably, an inhalation spray comprising a compound of formula I will be in the form of a solution, suspension or emulsion as exemplified above. The inhalation spray composition may further comprise an inhalable propellant of low toxicity. Suitable propellants include carbon dioxide or nitrous oxide. The dosage form of the compound of formula I will comprise from 0.01 % to 99% by weight of the active substance. Usually, dosage forms according to the invention will comprise from 0.1 % to about 10% by weight of the active substance. The compound of formula I may be administered together or sequentially with one or more other active substances known or believed to have anti- viral activity. Examples of such other active substances include AZT, acyclovir, ddC, ddA, trisodium phosphonoformate, castanospermine, rifabutin, ribaviran, bropirimine, phosphonothioate oligodeoxynucleotides, dextran sulfate, α-interferon and ampligen. BRIEF DESCRIPTION OF THE DRAWINGS Figure 1 is a graph showing the transformation of the compound of Example 5 ("Prodrug") into the compound of Example 20 of International Patent Application No. PCT/AU93/00103 ("Drug") in rabbit's blood in vitro. Figures 2 and 3 are graphs showing the transformation of Prodrug into Drug in vivo following intravenous and intramuscular (respectively) administration to a rabbit. BEST MODE OF CARRYING OUT THE INVENTION Methods for the preparation of compounds of formula (IB) wherein x and y are both 0, B is -CH(OH)- and R 50 6, R513, R542 and R 543 are hydrogen are described in the following Schemes 11 and 12: Scheme 1 1 R512 O R550 Rςm— N— C— C-'c— H H-N-N-R 502 H H H H R551 (i) iPrOH; 60-90°C;12 r Yield 70-90%, or (ii) Al 2 0 3 ; etheπ RT; 12-24hπ Yield 30-45% Scheme 12 (i) Nal DMF orAcCN; 1 r; RT; (ii) NaHC0 3 or tertiary amine; 2-12 hπ RT (iii) NaBH4; 30 min; RT Scheme 13 presents an example of a method of preparation of Examples 11 and 12, commencing with the product of Scheme 12 in which R 5Q I is benzyloxycarbonyl, R 5l2 is methoxycarbonyl, R5 50 and R 55 ι together form a 3,4-diazabicyclo[4.4.0]decane system and R 502 is tert-butoxy carbonyl: Scheme 13 Scheme 14 presents an example of a method of preparation of compounds of formula shown in Table 4 below, in which the solubilising group Px is P(O)(OH)H or P(O)(OH) 2 : Compositions of the third embodiment may be prepared by means known in the art for the preparation of pharmaceutical compositions including blending, grinding, homogenising, suspending, dissolving, emulsifying, dispersing and mixing of the compound of formula (I) together with the selected excipient(s), carrier(s), adjuvant(s) and/or diluent(s). In the method for the treatment of HIV viral infections in accordance with the fourth embodiment of the invention, a compound of the first embodiment will usually be administered orally or by injection. A suitable treatment may consist of the administration of a single dose or multiple doses of the compound of formula (I) or of a composition of the third embodiment. Usually, the treatment will consist of administering from one to five doses daily of the compound of formula (I) for a period of from one day to several years, up to the lifetime of the patient. Most usually, the treatment will consist of the administration of the compound of formula (I) for a period of from one day to one year. The administered dosage of the compound of formula I can vary and depends on several factors, such as the condition of the patient. Dosages will range from O.Olmg to 200 mg per kg. Usually, the dose of the active substance will be from O.Olmg to 25 mg per kg of body weight. Examples of dosage forms in accordance with the invention are as follows: 1. Tablet Compound of formula I 0.01 to 20 mg, generally 0.1 to lOmg Starch 10 to 20 mg Lactose 100 to 250 mg Gelatin 0 to 5 mg Magnesium stearate 0 to 5 mg Capsule Compound of formula I 0.01 to 20 mg, generally 0.1 to lOmg Glycerol 100 to 200 mg Distilled water 100 to 200 mg Saccharin 0 to 2 mg Methyl Paraben 1 to 2 mg Polyvinylpyrrolidone 0 to 2 mg Injectable solution Compound of formula I 0.01 to 20 mg, generally 0.1 to lOmg Sodium chloride 8.5 mg Potassium chloride 3 mg Calcium chloride 4.8 mg Water for injection, q.s. to 10 ml Elixir Compound of formula I 0.01 to 20 mg, generally 0.1 to lOmg Sucrose 100 mg Glycerol 2ml Carboxymethylcellulose 20mg Cherry flavour 2 mg Water q.s. to 10 ml EXAMPLES The following Examples describe the preparation of compounds according to the inventionand are intended to illustrate the invention. The Examples are not be construed as limiting in any way the scope of the present invention. Starting materials for the syntheses described in the following Examples are described in International Patent Application No. PCT/AU93/00103. In these Examples, melting points were taken on a hot stage apparams and are uncorrected. Proton and phosphorus NMR spectra were recorded at 100 MHz or 300MHz on Perkin Elmer R32 or Bruker EM 300 spectrometers, respectively, in CDCI3 unless otherwise stated. Chemical shifts for proton NMR are ppm downfield from tetramethylsilane; chemical shifts for P 31 NMR are ppm downfield from l,2-bis(diphenylphosphino)ethane external standard. Thin layer chromotography (TLC) was performed on silica gel 60-F254 plates (Merck). Compounds were visualized by ultraviolet light and/or 2% aqueous potassium permanganate solution. The composition (by volume) of the TLC solvent systems were (A) hexane/ethyl acetate 3:2, and (B) concentrated N^OH/isopropanol 1:3. Example 1 4S,5S-5,6-Dibenzyl-l,2-(cis-l,2-cyclohexane)dimethyl-4-hydroxy-7-oxo-perhydro- 1,2,6-triazepine Step A: 4S, 5S-5-benzyl-l, 2-(cis-l, 2-cyclohexane)dimethyl-4-t-butyldimethylsilyloxy-7-oxo- erhydro-l,2,6-triazepine: Hydrogen chloride gas was bubbled through the solution of 0.51 g (1.26 mmol) of. cis-l,6-3-t-butoxycarbonyl-4-[(2S,3S)-2-hydroxy-3-amino-4- phenylbutyl]-3,4-diazabicyclo[4.4.0]decane (isomer having Rf (A) = 0.16 when eluted with 8% methanol in dichloromethane) in 10 ml of 1 % solution of methanol in methylene chloride for 30 min at room temperature. After purging the excess of hydrogen chloride with nitrogen gas the solvent was removed under reduced pressure to give 0.42 g (100% yield) of the hydrochloride salt of cis-l,6-4-[(2S,3S)-3-amino-2-hydroxy-4-phenylbutyl]- 3,4-diaza-bicyclo[4.4.0]decane as a hygroscopic, white solid. This was dissolved in 1 ml of dry DMF and 0.114 g (1.68 mmol) of imidazole and 0.21 g (1.38 mmol) of t- butyldimethylsilyl chloride were added under nitrogen. The resulting mixture was stirred overnight at room temperamre and evaporated to dryness in vacuo. The residue was diluted to 20 ml with ethyl acetate, washed with samrated sodium bicarbonate and dried over anhydrous potassium carbonate and filtered off. The filtrate was evaporated to dryness under reduced pressure and the residue was dissolved in 20 ml of dry dioxane. To this, 0.204 g (1.26 mmol) of l,l'-carbonyldiimidazole was added and the resulting mixmre was stirred for 24 hrs at room temperamre. After evaporation of the solvent under reduced pressure the residue was diluted to 15 ml with ethyl acetate and washed with water (3x) and samrated aqueous sodium chloride solution, and then dried over anhydrous magnesium sulfate. Evaporation of the solvent under reduced pressure and purification of the residue by column chromatography (silica gel; hexane/ethyl acetate 3:2) gave 0.095 g (17% yield) of the title compound, melting at 145 - 146°C; R f (A) = 0.43; NMR 0.07, 0.09 (s,s 6H, CH 3 ); 0.94 (s, 9H, t-butyl CH 3 ); 1.2 - 2.0 (m, 10H, cyclohexane CH 2 , CH); 2.5 - 2.8 (m, 4H, CH 2 -3, benzyl CH 2 ); 3.2 - 3.7 (m, 4H, dimethyl CH 2 ); 3.9 - 4.0 (m, 3H, CH-4,5, NH); 7.1 - 7.32 (m, 5H, aromatic). Step B: 4S, 5S-5, 6-dibenzyl-l, 2- (cis-1, 2-cyclohexane)dimethyl-4-t-butyldimethylsilyloxy- 7- oxo-perhydro-l,2,6-triazepine: 4.5 mg (0.15 mmol) of 80% dispersion of sodium hydride in mineral oil was added to a solution of 0.0665 g (0.15 mmol) of the product of Step A in 0.2 ml of dry DMF at room temperature. After stirring for 30 min at room temperamre, 0.0179 ml (0.15 mmol) of benzyl bromide was then added. The resulting mixmre was stirred overnight, then diluted to 15 ml with ethyl acetate and washed with water, samrated aqueous sodium chloride solution and dried over anhydrous magnesium sulfate. Evaporation of the solvent under reduced pressure and purification of the residue by column chromatography gave 0.029 g (36% yield) of the title compound as a heavy syrup; R f (A) = 0.77; NMR -0.35, -0.18 (s, s, CH 3 ); 0.8 (s, 9H, t-butyl CH 3 ); 1.2 - 2.2 (m, 10H, cyclohexane CH 2 , CH); 2.56 - 4.18 (m, 12H, benzyl CH 2 , dimethyl CH 2 , CH 2 -3, CH-4,5); 6.8 - 7.4 (m, 10H, aromatic). Step C: 4S, 5S-5, 6-Dibenzyl-l, 2- (cis-1, 2-cyclohexane)dimethyl-4-hydroxy- 7-oxo-perhydro- 1,2,6-triazepine: A mixmre of 29 mg (0.0543 mmol) of the product of Step B and 0.0426 g (0.163 mmol) of tetrabutylammonium fluoride hydrate in 1 ml of anhydrous acetonitrile was stirred at 45±5°C for 3 hrs and evaporated to dryness. The residue was purified by column chromatography (silica gel, hexane/ethyl acetate 3:2) to give 0.019 g (86% yield) of the title compound as a colourless foam; R f (A) = 0.26; NMR 1.2 - 2.1 (m, 18H, cyclohexane CH 2 , CH, OH, 3.5 x H 2 O); 2.6 - 4.0 (m, 11H, benzyl CH 2 , dimethyl CH 2 , CH 2 -3, CH-5); 4.83 (m, 1H, CH-4); 7.0 - 7.4 (m, 10H, aromatic). Example 2 4S,5S-l,5,6,Tribenzyl-2-isopropyl-4-hydroxy-7-oxo-perhydro-l,2,6-triazepine Step A: 4S, 5S-5-benzyl-2-isopropyl-4-t-butyldimethylsilyloxy-7-oxo-perhydro-l, 2, 6- triazepine: When t-butyl 3-isopropyl-3-[(2S,3S)-3-amino-2-hydroxy-4-phenylbutyl]- carbazate was substimted for cis-1, 6-3-t-butoxycarbonyl-4-[(2S, 3S)-2-hydroxy-3-amino- 4-phenylbutyl]-3,4-diazabicyclo[4.4.0]decane in Step A of Example 1 the identical process afforded the title compound in 20% overall yield; melting point = 131 - 132°C (hexane); R f (A) = 0.18; NMR 0.10, 0.11 (s, s, 6H, silyl CH 3 ); 0.95 (s, 9H, t-butyl CH 3 ); 1.1 - 1.35 (m, 6H, isopropyl CH 3 ); 2.8 - 3.2 (m, 5H, CH 2 -3, CH-5, benzyl CH 2 ); 3.45 (m, 1H, isopropyl CH); 4.18 (m, 1H, CH-4); 4.41 (m, 1H NH-6); 5.63 (s, 1H, NH- 1); 7.1 - 7.4 (m, 5H, aromatic). Step B: 4S, 5S-1, 5, 6-tribenzyl-2-isopropyl-4-t-butyldimethylsilyloxy- 7-oxo-perhydro-l , 2, 6- triazepine: A mixture of 0.07 g (0.185 mmol) of the product of Step A and 0.012 g (0.371 mmol) of sodium hydride in 0.2 ml of dry DMF was stirred for 30 min at room temperature, then 0.0441 ml (0.371 mmol) of benzyl bromide was added. The resulting mixmre was stirred overnight and worked up as described in Step B of Example 1. The purification of the crude product by column chromatography (silica gel, hexane/ethyl acetate 3:2) gave 0.031 g (30% yield) of the title compound as a colourless syrup; Rf (A) = 0.74, NMR -0.28, -0.22 (s,s, 6H, silyl CH 3 ); 0.8 (s, 9H, t-butyl CH 3 ); 1.0 - 1.35 (m, 6H, isopropyl CH 3 ); 2.35 - 3.3 (m, 5H, CH 2 . 3 , CH-5, 5-benzyl CH 2 ); 3.45 - 3.82 (m, 2H, isopropyl CH, CH-4); 4.0 - 5.38 (m, 4H, 1,6-benzyl CH 2 ); 6.6 - 7.8 (m, 15H, aromatic). Also, the fractions with Rf (A) = 0.63 were combined and evaporated to dryness under reduced pressure to give 0.061 g (70% yield) of 4S,5S-5,6-dibenzyl-2-isopropyl-4-t-butyl- dimethylsilyloxy-7-oxo-perhydro-l,2,6-triazepine as a colourless solid; NMR 0.11 (d, 6H, silyl CH 3 ); 0.93 (s, 9H, t-butyl CH 3 ); 1.24 (m, 6H, isopropyl CH 3 ); 2.4 - 3.4 (m, 5H, CH 2 -3, CH-5, 5-benzyl CH 2 ); 3.75 (m, 1H, isopropyl CH); 4.0 - 4.7 (m, 3H, CH-4, 6-benzyl CH 2 ); 5.05 (m, 1H, NH); 7.0 - 7.7 (m, 15H, aromatic). Step C: 4S, 5S-1.5, 6-Tribenzyl-2-isopropyl-4-hydroxy-7-oxo-perhydro-l, 2, 6-tήazepine: When the title compound of Step B was substimted for 4S,5S-5,6-dibenzyl-l,2-(cis-l,2- cyclohexane)-dimethyl-4-t-butyldimethylsilyloxy-7-oxo-perhydro-l ,2,6-triazepine in Step C of Example 1 , the identical process afforded the title compound with 98 % yield as a foam; Rf (A) = 0.68; NMR (CDC1 3 ) 1.07, 1.19 (d, d, 6H, isopropyl CH 3 ); 1.58 (s, 1H, OH); 2.6 - 3.15 (m, 5H, CH 2 -3, CH-5, 5-benzyl CH 2 ); 3.2 - 5.3 (m, 6H, isopropyl CH, CH-4, 1,6-benzyl CH 2 ); 6.8 - 7.6 (m, 15H, aromatic). Example 3 4S,5S-5,6-dibenzyl-2-isopropyl-4-hydroxy-7-oxo-perhydro-l,2,6-triazepine When 4S,5S-5 ,6-dibenzyl-2-isopropyl-4-t-butyldimethylsilyloxy-7-oxo-perhydro-l ,2,6- triazepine was substimted for 4S,5S-l,5,6-tribenzyl-2-isopropyl-4-t-butyldimethylsilyloxy- 7-oxo-perhydro-l,2,6-triazepine in Step C of Example 2 the identical process afforded the title compound in 88% yield; melting point = 191 - 193°C; Rf (A) = 0.17; NMR (DMSO-d 6 , 80°C) 2.5 - 3.0 (m, 4H, CH 2 -3, 5-benzyl CH 2 ); 3.28 (m, IH, CH-5); 3.6 (m, IH, CH-4); 3.8 (m, IH, isopropyl CH); 4.2 - 4.7 (m, 3H, 6-benzyl CH 2 ; OH); 5.41 (m, IH, NH); 7.0 - 7.4 (m, 10H, aromatic). Example 4 t-Butyl 3-isopropyl-3-[(2S, 3S)-2-phosphitooxy-3-(N-quinaldoyl-L- asparaginyl)amino-4-phenylbutyl carbazate To a mixmre of 0.4 g (0.67 mmol) of t-butyl 3-isopropyl-3-[(2S, 3S)-2-hydroxy-3- (N-quinaldoyl-L-asparaginyl)amino-4-pheny lbutyl carbazate and 0.12 g (1.47 mmol) of anhydrous phosphorous acid in 1.5 ml of anhydrous pyridine was added 0.28 g (1.4 mmol) of dicyclohexylcarbodiimide at room temperamre under nitrogen, with stirring. After stirring for 2 hours at 60°C, the solvent was evaporated under reduced pressure and the residue was treated with 28 ml of 0.1 ml aqueous sodium bicarbonate and vigorously stirred for 1 hour at room temperamre. The precipitate was filtered off and washed with water and the filtrate was acidified to pH ~ 1.5 with concentrated hydrochloric acid. The product was taken up by extraction with ethyl acetate (3 x 50 ml), and the organic phase was dried over anhydrous magnesium sulfate. Evaporation of the solvent gave 0.42 g (95% yield) of the title product as a colourless solid; R f (B) = 0.62; H*NMR (CDC1 3 ): 1.08 (m, 6H, isopropyl CH 3 ); 1.41 (s, 9H, t-butyl CH 3 ); 2.7 - 4.8 (m, 14H, asn CH 2 , butyl CH 2 -1, 4; CH-2,3; isopropyl CH; P-OH x 2H 2 O); 5.12 (m, IH, asn CH); 5.89 (s, 0.5 H, PH); 6.2 - 8.5 (m, 15.5 H, aromatic, amide NH, 0.5 PH); 9.02 (m, IH, asn NH); P 31 NMR (CDC1 3 ) 14.99 (J P . H = 636 Hz). Example 5 t-Butyl 3-isopropyl-3-[(2S, 3S)-2-phosphonooxy-3-(N-quinaldoyl-L- asparaginyl)amino-4-phenylbutyl carbazate A suspension of 0.4 g (0.6 mmol) of the product of Example 4 in 2 ml of hexamethyldisilazane was stirred for 45 min at 120 + 5°C. At this point the reaction mixmre became homogeneous. To this 0.3 ml of bis(trimethylsilyl)peroxide (Cookson, P.G et al., J. Organometal. Chem. , 1975, 22, C31) was added and stirring was continued for 1 hour at the above temperature. The reaction mixture was cooled to room temperamre, then evaporated to dryness in vacuo. The residue was dissolved in 20 ml of methanol, evaporated to dryness under reduced pressure and redissolved in 12 ml of 0.1 ml aqueous sodium bicarbonate. The resulting mixmre was acidified to pH ~ 1.5 with concentrated hydrochloric acid, samrated with sodium chloride and extracted with ethyl acetate (3 x 50 ml). The combined organic phase was dried over anhydrous magnesium sulfate and evaporated to dryness to give 0.39 g (96% yield) of the title compound as a colourless solid; R (B) = 0.07; H i NMR (CDC1 3 ): 1.2 (m, 6H, isopropyl CH 3 ); 1.4 (s, 9H, t-butyl CH 3 ); 2.8 - 4.2 (m, 8H, asn CH 2 butyl CH 2 -1,4, CH-3, isopropyl CH); 4.2 - 6.4 (m, 5H, asn CH, butyl CH-2, NH, POH); 6.5 - 8.4 (m, 14H, aromatic, NH); 8.78 (m, 2H, NH); P^lNMR (CDC1 3 ) 9.6 (s). Example 6 cis-l,6-3-t-Butoxycarbonyl-4-[(2S, 3S)-2-phosphitooxy-3-(N-quinaldoyl-L- asparaginyl)amino-4-phenylbutyl]-3,4-diaza-bicyclo[4.4.0]decane When cis-1, 6-3-t-butoxycarbonyl-4-[(2S, 3S)-2-hydroxy-3-(N-quinaldoyl-L- asparaginyl)amino-4-phenylbutyl]-3,4-diaza-bicyclo[4.4.0]decane is substituted for t-butyl 3-isopropyl-3-[(2S, 3S)-2-hydroxy-3-(N-quinaldoyl-L-asparaginyl)amino-4-phenylbutyl- carbazate in Example 4, the identical process affords the title compound in 89% yield, as a colourless solid; R f (B) = 0.64; H NMR (CDC1 3 ): 1.1 - 1.8 (m, 19H, t-butyl CH 3 , decane CH 2 -7,8,9,10, CH-1,6); 2.12 (m, IH, butyl CH-3); 2.6 - 5.1 (m, 19H, asn CH 2 , CH, butyl CH 2 -1,4, CH-2, decane CH 2 -2,5, POH x 2.5 H 2 O); 6.1 - 8.4 (m, 15H, amide NH, PH, aromatic); 9.08 (m, IH, asn NH); P 31 NMR (CDC1 3 ) 16.43 (J PH = 700 Hz). Example 7 cis-l,6-3-t-Butoxycarbonyl-4-[(2S, 3S)-2-phosphonooxy-3-(N-quinaldoyl-L- asparaginyl)amino-4-phenylbutyl]-3 ,4-diaza-bicyclo[4.4.0]decane When the product of Example 6 is substimted for t-butyl 3-isopropyl-3-[(2S, 3S)-2- phosphitooxy-3-(N-quinaldoyl-L-asparaginyl)amino-4-phenylbutyl carbazate in Example 5, the identical process affords the title compound in 83% yield, as a colourless solid; R f (B) = 0.12; H*NMR (CDC1 3 ): 1.1 - 2.4 (m, 20H, t-butyl CH 3 , decane CH 2 -7,8,9,10, CH-1,6, butyl CH-3); 2.7 - 3.9 (m, 9H, asn CH 2 , butyl CH 2 -1,4, CH-2, decane CH 2 -5); 5.1 (m, IH, asn CH); 6.1 - 8.3 (m, 21H, amide NH, aromatic, POH x 2.5 H 2 O); 9.05 (m, IH, asn NH); P *NMR (CDC1 3 ) 10.5 (s). Other representative compounds in accordance with the invention are described in Tables 1 to 5. Other compounds in accordance with the invention are substances in 5 which a hydroxyl, amino or mercapto group is any of the compounds described in the Examples and disclosures of the following, has been derivatised with a solubilising group Px as defined herein: US Patent Nos. 5,116,835, 5,126,326; 5,132,400; 5,145,951; 5,198,426; 5,212,157; 5,215,968; 5,221,667; 5,250563; 5,268,361; 5,294,720; and 5,296,604; International io Patent Application Nos. 90/09191; 91/08221; 91/10442; 92/15319 and 92/21696; European Patent Application Nos. 0574135; 0528242; 0519433 and 0432595 and Australian Patent Application Nos. 35700/89; 42308/89; 45665/89; 46115/89; 53716/90 63221/90; 66334/90; 71319/91; 71320/91; 71323/91; 77326/91; 81910/91; 82054/91 88900/91; 82313/91; 83234/91; 83206/91; 85877/91; 87309/91; 87409/91; 87594/91 15 88900/91; 89941/91; 90531/91; 90851/91; 90925/91; 91223/91; 91251/91; 91332/91 91790/92; 10812/92; 18355/92; 19373/92; 21944/92; 22889/92; 24129/92; 24690/92 26424/92; 31628/93; 35165/93; 35621/93; 37160/93; 38808/93; 41230/93; 41659/93 44930/93 and 49072/93, the disclosures of each of which are incorporated herein by reference. 20 Example S In Vivo Removal of Phosphono Group Solutions: The product of Example 5 was converted quantitatively into the corresponding disodium salt by treatment of the free acid with 2 equiv. of 0.2 M sodium bicarbonate and lyophilization of the resulting solution. The stock solutions of the disodium salt of the 25 product of Example 5, for blood and animal experiments, were prepared in sterile water. Analyses: Reverse phase analyses (HPLC) were performed on Waters ternary gradient liquid chromatograph equipped with 996 diode array detector set at 238 nm. Separations were achieved on Alltima RP-18 (250 x 4.6 mm, i.d., 5 μ particles), with the flow rate of 1 ml/min. The isocratic mobile phase composition used for analyses consisted of 40% of 30 0.1 % aqueous trifluoroacetic acid (TFA) and 60% of acetonitrile containing 0.1 % TFA and 10% water. The retention time of the product of Example 5 (referred to below as "Prodrug") was in the range of 3.6 - 3.9 minutes and the retention time of t-butyl 3-isopropyl-3-[(2S, 3S)-2-hydroxy-3-(N-quinaldoyl-L-asparaginyl)amino-4-phenylbutyl -carbazate (referred to below as "Drug) was about 6.2 minutes. Detector response was 35 linear from 0.5 to 120 μM for Prodrug and 0.05 to 50 μM for Drug. Standards and Sample Processing: The standards were prepared by serial dilution of Prodrug or Drug in rabbit blood collected into heparinised tubes. Blood samples were transferred into vials containing 150 units of heparin and stored on ice until processed. The blood samples were then separated by centrifuging at 6000 rpm for 10 min. The plasma samples were frozen and stored at -20°C until they were analysed. Plasma preparation for HPLC analysis: An equal volume (100 μL) of thawed plasma and acetonitrile was stirred with a vortex mixer and allowed to stand at room temperature for 5 minutes, then centrifuged at 14000 rpm for 10 minutes. Samples of the supernantant (50 μL) were injected into the chromatograph. Transformation of Prodrug into Drug by Blood was established by measurement of prodrug and drug concentrations in plasma following the prodrug incubation in whole rabbit's blood (100 μM) at 36°C for 19 hours. Fig. 1 shows the concentrations of prodrug and drug under these conditions over 19 hours. Transformation of Prodrug into Drug after intravenous (IV) administration of prodrug (9.2 mg/kg) to rabbit was established by measurement of prodrug/drug concentrations in plasma over 120 min. The formulated product, containing 30 mg/ml of prodrug, was well tolerated by the rabbit. The plasma profiles of prodrug and drug disappearance are shown in Fig. 2. Transformation of Prodrug into Drug after Intramuscular (IM) administration of prodrug (7.9 mg/kg) to rabbit was established by measurement of drug concentrations in plasma over 330 min. The formulated product, containing 30 mg/ml of prodrug was well tolerated by the rabbit. The time dependence of the plasma concentration of the drug are shown in Fig. 3. When prodrug was administered to a dog orally at a dose of 20mg/kg, the blood plasma concentration of drug was found to be 0.044, 0.141, 0.189, 0.172, 0.164, 0.132, 0.089 and 0.060 μM, respectively, after 5, 15, 30, 47, 63, 93, 124 and 155 minutes. When prodrug was administered to a second dog orally at a dose of lOmg/kg, the blood plasma concentration of drug was found to be 0.137, 0.371, 0.297, 0.242, 0.176, 0.11, 0.071, and 0.050 μM, respectively, after 5, 15, 30, 45, 60, 94, 123 and 154 minutes. TABLE 1 Compounds of formula Compound R501 R 506 B A* R 550 RSSI R 502 No. CΛ S 9. BzOC(O)- Et -CH, -(CH 2 ) 4 - t-BuOC(O)- 10. Me -CHπ Et H -SO 2 Me TABLE 1 (CONT.) Compound R 501 R 506 A B A* R 550 RS51 R 502 No. OH OH 14. Ac Ph -CH 2 CH 2 - I CO 2 Me Pr H -C — -C-CH 2 - I I CO 2 Me H O 15. MeS(O) iPr -CH 2 CHF- HC-CH -CHFCH 2 - Me Bz -S(O) 2 Ph CΛ CΛ 16. MeS(O) 2 Pr -CH(Me)- -CH(OTHP)- -S(O)Me TABLE 1 (CONT.) A B A* R 550 R551 R 502 Bz -(CH 2 ) 3 C(O)- Me 2 N 25. Ph n-Bu Ph TABLE 1 (CONT.) Compound R 501 R 506 A B R 550 RSSI R 502 No. TABLE 1 (CONT.) Compound R501 R 506 A B A* R 550 R 551 R 502 No. TABLE 1 (CONT.) Compound R 501 R 506 A B A* R 550 RSSI R 502 No. Compound R 501 R 506 A* R 550 RS51 R 502 No. A* R 550 RSSI R 502 -CH 2 - Bz H t-BuOC(O)- -CH 7 O c H t-BuOC(O)- -CH, -CH / £ -CH,— BuOC(O)- TABLE 1 (CONT.) Compound R 501 R 506 A B A* R 550 Rssi R 502 No. Compound R 501 R 506 A* R 550 R 551 R 502 No. H TABLE 1 (CONT.) Compound R 501 R 506 A B A* R 550 Rssi R 502 No. 72 TABLE 1 (CONT.) Compound R 501 R 506 A B A* R 550 R 551 R 502 No. TABLE 1 (CONT.) R 506 A B A* R 550 R 551 R 502 IΛ a a a a a * < IΛ Pi a a a a *N O u o 3 PQ IΛ a a < a a u u tf a a af IΛ IΛ a a a a u a u a u a u a u tf a a O e 3 Os o o CN CO O o y Compound R 501 R 506 R 550 RS51 R 502 No. H i-Pr H t-BuOC(O)- 108. PhCO -CH(OH)- -CH(OH)- -CH(OH)- IΛ IΛ IΛ a o y a u Ό c 3 ON o ε o z y TABLE 2 Compounds of formula W-(A) n -B-(A*) m -V Compound w (A)„ B (A*) m No TABLE 2 (CONT.) Compound w (A) n B (A*) m No TABLE 2 (CONT.) Compound W (A) n B (A*), m No 119. H 3 C- V-S(0) 2 -NHC(0)NH- 122. -CN 123. MeOC(O)- TABLE 2 (CONT.) Compound W (A) n B (A*) m No TABLE 2 (CONT.) Compound W (A) n B (A*), m No TABLE 2 (CONT.) Compound W (A)„ B (A*) m TABLE 2 (CONT.) Compound W (A)„ B (A*); m No Pr C Me Table 3 Examples of Other Compounds of Formula (I) 141. 142. 143. 144. 145. O Table 3 (cont.) 146. O 147. 148. 149. 150. Table 3 (cont.) 151. 152. 153. 154. 155. Table 3 (cont.) 156. 157. 158. 159. 160. 161. Table 3 (cont.) 162. Table 3 (cont.) 167. 1 Table 3 (cont.) 171. 172. 173. 174. 175. Table 3 (cont.) 176. 177. 178. Table 3 (cont.) 179. 180. 181. TABLE 4 Compounds of formula Compound R 501 R 506 R 12 Px R 550 R551 R 502 No. 187. Z H Bz HP(O)(OH) Bz H Boc o o 188. z H Bz _x>. C 6 H U H Boc H 189. z H Bz P(O)(OH) 2 -(CH 2 ) 4 - Boc Compound R 501 R 506 R551 R 502 192. Z-Val H H Z-Val 193. Z-Val H H Boc-Val H Val 196. Z-Val H H MC-Gly-Val 197. Z-Val H (p-F)Bz TABLE 4 (cont.) Compound R 501 R 506 Rl2 Px R 550 R 551 R 502 No. 198. Z-Val H (p-F)Bz (p-F)Bz H H 203. Z-Val H Bz TABLE 4 (cont.) Compound R501 R 506 Rl2 Px R 550 R 551 R 502 No. 209. Z-Val H (p-F)Bz TABLE 4 (cont.) Compound RSOI R 506 Rl2 Px R550 R551 R 502 No. 221. QC-Asn H Bz P(O)(OH) 2 i-Pr H TABLE 4 (cont.) Compound RSOI R 506 Rl2 Px R550 R551 R 502 No. 228. QC-Asn H Bz i-Pr H -C(O)Bu l H QC-Val Boc 236. QC-Thr H Bz P(O)(OH) 2 TABLE 4 (cont.) R 506 Rl2 Px R 550 R551 R502 H Bz P(O)(OH) 2 H H Bz P(O)(OH) 2 Boc ^Ph H Bz P(O)(OH) 2 Bz H BzC(O)-Val 243. PC-Val H Bz PC-Val 244. PC-Val H Bz PC-Val 245. PC-Val H Bz PC-Val 246. PC-Asn H Bz Boc TABLE 4 (cont.) Compound R 501 R 506 R 12 Px R 550 RS51 R 502 No. TABLE 4 (cont.) Compound R501 R 506 R12 Px R 550 R 551 R 502 No. 262. MC-Val H Bz NO 7 i-Pr H H TMC-Val H Boc H Boc TABLE 4 (cont.) Compound R501 R 506 Rl2 Px R550 R551 R 502 No. 268. TFA H Bz H Bz H Ac H Bz H Ac-Val H Bz H Ac-Val H Bz H Ac-Val H Bz H Ac-Val H Bz P(O)(OH) 2 CH 2 C 6 H π H Ac-Ile H Bz P(O)(OH) 2 i-Pr H Boc 278. H Bz P(O)(OH) 2 i-Pr H Boc H'N ] TABLE 4 (cont.) Compound R 501 R 506 Rl2 P R 550 RSSI R 502 No. 279. H Bz P(O)(OH) 2 i-Pr H Boc 281. 282. 283. TABLE 4 (cont.) Compound R 501 R 506 R 12 Px R 550 Rssi R 502 No. Boc 293. ZAsn H Bz P(O)(OH) 2 i-Pr Boc TABLE 5 Further examples of compounds of formula (I) 294. 5 295. 296. H 2 297. 0 298. 299. 5300. 301. 0 303. 304. 5 305. 306. 309. 310. 5 311. 312. 313. 0 314. 315. 5 317. CLAIMS 1. A compound of the general formula (I) or a pharmaceutically acceptable salt or prodrug thereof: W-(A) n -B-(A*) m -V (I) wherein W is selected from the group consisting of R X-, R^-X*-, -Y*, -CN, -N=CR 5 R 5 *, -C(R 5 )=NR 3 , -C(R 5 )=NOR 3 , -C(NR 3 R 4 )=NR 5 **, -C(D)OR 3 , -C(D)SR 3 and -C(D)NR 3 R 4 , wherein Y* is as defined below, R 1? R 3 and R 4 are independently selected from the group consisting of R and a solubilising group Px which is labile in vivo, wherein R is selected from the group consisting of hydrogen, R 20 , wherein R Q is selected from the group consisting of optionally substituted (C 1 -C 18 )alkyl, optionally substituted (C -C 18 )alkenyl, optionally substituted (C -C 18 )alkynyl, optionally substituted (C 3 -C 18 )cycloalkyl, optionally substituted (C 3 -C 18 )cycloalkyl(C r C 18 )alkyl, optionally substituted (C 3 -C 18 )cycloalkyl(C 2 -C 18 )alkenyl, optionally substituted (C 3 -C 18 )cycloalkyl(C 2 -C 18 )alkynyl, optionally substituted (Cg-C^aryl, optionally substituted (C 6 -C 24 )aryl(C 1 -C 18 )alkyl, optionally substituted (C 6 -C 24 )aryl(C -C 18 )alkenyl, optionally substituted (C 6 -C 24 )aryl(C 2 -C 18 )alkynyl, optionally substituted (C 1 -C 18 )acyl, optionally substituted heterocyclic, optionally substituted heterocyclic(C r C 18 )alkyl, optionally substituted heterocyclic(C 2 -C 18 )alkenyl, and optionally substituted heterocyclic(C 2 -C 18 )alkynyl C(D)OR 21 , C(D)SR 21 , C(D)NR 21 R 22 , C(NR 21 )R 22 , C(NR 21 )OR 22 , and C(NR 21 )NR 22 R 23 , wherein R 21 , R 22 and R 23 independently are selected from hydrogen and R 20 as previously defined, or R 21 and R 22 together, or R 22 and R 23 together form a

Claims: saturated or unsaturated cyclic, bicyclic or fused ring system as defmed herein, or R 3 and R 4 , when present, together form a saturated or unsaturated cyclic, bicyclic or fused ring system as defined herein, D is selected from O and S, X is selected from the group consisting of Y, S(O) and S(O) wherein Y is as defined below, X* is selected from the group consisting of NR 10 , O and S, wherein R 10 has the meaning of Rg as previously defmed, R j * is selected from the group consisting of Rx. as previously defmed, P(O)(OR 7 )R 8 , S(O) z OR 7 and S(O) z NR 7 R 8 , wherein z is 1 or 2 and R 7 and Rg independently have the meaning of R 2 o as previously defmed, or R 7 and R 8 together form a saturated or unsaturated cyclic, bicyclic or fused ring system as defined herein, R 5 and R 5 * are independently selected from the group consisting of H, CF 3 , C(D)OR 103 , C(D)SR 103 C(D)NR 103 R 104 and R 20 as previously defmed, wherein D is as previously defined, and wherein R^ and R 104 have the meaning of Rβ as previously defined, or R 103 and R 104 together form a saturated or unsaturated cyclic, bicyclic or fused ring system as defined herein, and R 5 ** is selected from hydrogen and R 2Q as previously defined; n is 0-6; m is 0-6 and n+m > 1; A at each occurrence is independently selected from the group consisting of » and a residue of a naturally occurring or synthetic amino acid; A* at each occurrence is independently selected from the group consisting of and a residue of a naturally occurring or synthetic amino acid; wherein R 12 *, R j3 *, R9 and R9* are independently selected from the group consisting of F, Cl, Br, I and R5 as previously defined, Rn has the meaning of R^ as previously defmed, R 12 has the meaning of R β as previously defmed, R 13 is selected from the group consisting of F, Cl, Br, I, Rβ as previously defmed, and R 2 oo, wherein R 2 QO is selected from the group consisting of CN, NCO, NCS, OCN, SCN, N 3 . OReo, SROO> NRfioRβj, D 1 C(D 2 )R 60 , D 1 C(D 2 )D 3 R 60 , D 1 C(D 2 )NR 60 R 6 ι, NR 60 C(D 1 )R 61 , NR 60 C(D 1 )D 2 R 61 , NR 60 C(D 1 )NR 61 R 62 , NReoORe!, amidino, guanidino, S(O)R6 0 , S^^D^o, S(O)NR 60 R 61 , S^NRgnRg ! , D j S^Rg Q , DjS^ORg Q , D 1 S(0)NR β oR 61 , P(D 1 )(D 2 R 60 )R 61 , P(D 1 )(D 2 R 60 )D 3 R 61 , P(D 1 )(D 2 R 60 )NR 61 R 62 , D 1 P(D 2 )(D 3 R 60 )R 61 , D 1 P(D 2 )(D 3 R 60 )D 4 R 61 , D 1 P(D 2 )(D 3 R 60 )NR 61 R 62 , D 1 P(D 2 )R 60 R 61 , NR 60 NR 61 R 62 and ONRggR όl ' wherein Dj, D 2 , D 3 and D 4 independently have the meaning of D as previously defmed, and Q, R $ ι and Rg 2 independently have the meaning of Rβ as previously defmed or any two or more of Rβo. Rβi and Rβ 2 form part of a saturated or unsaturated cyclic, bicyclic or fused ring system as defined herein, or R 1 and R^ 3 together are selected from the group consisting of =O, =S, / R∞ = C i =NOR 60 , =NR 60 , -OQO-, -SQS- and -SQO-, wherein Q is optionally substituted (C 1 -C 1 )alkylidene as defmed herein and Rgo is as previously defined, and L is selected from the group consisting of a bond, D D II II — C— N — — N— C — I I R11 R11 — O— — S— — S(0) z — — N— — S(O)z-N— — N-S(0)z- — N-S(0) z N— Ri 1 Ri ι Ri ι Ri ι Ri 1 * D D D II II II — N-C— N— — S(0)z-N-C— — S(0)z-N-C— N— I I ' I I I R11 R11* Rn R11 Rn* D D NR11 II II R13 * II -D*-C— N- -N— C-D*- -C— N — I I I '^ R11 R11 N- R11 * -CH 2 - and -CH -CH 2 -, wherein Rn and D are as previously defined, Rn* and D* have the meaning of Rn and D respectively, and z is 1 or 2; R 13** is F, Cl, Br, ORgg or NRgnRβo wherein R^ and Rg ! are as previously defined, B is selected from the group consisting of wherein R 203 and R 2 o 3 * independently have the meaning of R β as previously defined, R 14 * and R 14 ** are independently selected from the group consisting of hydrogen, R 0 as previously defined, CF 3 , C(D*)OR 40 , C(D*)NR oR 4 ι, wherein R 40 and R 41 independently have the meaning of R 21 and R 22 as previously defined or R Q and R 41 form part of a saturated or unsaturated cyclic, bicyclic or fused ring system as defined herein, R 1 is selected from the group consisting of F, Cl, Br, I, R 1 * as previously defined and R 2 oo as previously defined, R 17 and R 17 * independently have the meaning of R as previously defined, D* has the meaning of D as previously defined, Z is a saturated or unsaturated (C 2 -C 4 )alkylidene radical which is optionally substituted with one or more groups selected from F, Cl, Br, I and Rj * as previously defined, Z* is a saturated or unsaturated (C 1 -C 3 )alkylidene radical which is optionally substituted with one or more groups selected from F, Cl, Br, I and R 14 * as previously defined, M j is selected from the group consisting of OR 15 , SR 15 and NR^R^, wherein R15 is selected from the group consisting of: Px as previously defined, Rβ as previously defined, , , , wherein Px and D are as previously defined and R is H or C r C 4 alkyl, and a glycosyl radical which is derived from a synthetic or naturally occurring aldose, ketose, deoxyaldose, deoxyketose, aminoaldose, aminoketose or an oligosaccharide thereof, and Rj 7 is as previously defined, or R 15 and R^ 7 together form a samrated or unsaturated cyclic, bicyclic or fused ring system as defined herein, M and M* are independently selected from the group consisting of M j as previously defined, OCN, SCN, YR 2 , Y* and N=CR 30 R 31 , wherein Y, Y* and R 2 are as defmed below, and R 30 and R 31 independently have the meaning of R 2 Q as previously defined, M 2 is selected from the group consisting of R 14* as previously defined, -CR 30 *=Y** and -CR 30 *=NR 17 *, where Y** is as defined below, R 30 * has the meaning of R 2 o as previously defined, and R^ 7 * is as previously defined, Rig and R^ independently have the meaning of R 2 o as previously defined or R 18 and R^ together form part of a samrated or unsaturated cyclic, bicyclic or fused ring system as defined herein, and R 1 * and R 19 * together form part of a samrated or unsaturated cyclic, bicyclic or fused ring system as defined herein; V is selected from the group consisting of YR 2 , Y* and C(R 30 )= Y**, wherein Y is absent or is selected from the group consisting of: O o- II — S-N— -N=N— — N=N- — N=N- I + + R50 O O o o -S— N— -N-S — — N— S- II I I II — o-s- II O R50 R • 5- 0 R 50 O o o o o 0 II II — s-o — — s— s- — o— s — — s-o — II II o o O O O Y 11 11 — S— S — — S— S — — P— N — — O— P— N — O R51O R50 R51O R50 O O O o II II II II — N— P— — N-P-O— — P— O- — O— P — I I I I I I R50OR51 R50OR51 OR51 OR51 O O o o II II II II — P— N — — N— P— — P-O— — O— P— I I I I I I and R 51 O R50 R50OR 5 1 D ** R 52 D ** R 52 o II — o-p-o- D ** R 5 ι » wherein D** is selected from the group consisting of a bond, O, S and NR 50 , R 50 has the meaning of Rβ as previously defined, R 51 has the meaning of R 15 as previously defined and R 52 has the meaning of R 20 as previously defined, or R 50 and R 51 , when present, together form part of a saturated or unsamrated cyclic, bicyclic or fused ring system as defined herein, and R 2 has the meamng of R as previously defined, Y* is selected from the group consisting of R33 — N-N-R * — N-N=C — N-O-R 2 * — O-N-R 2 * 1 1 ' N R3 ' ' R50 R5I ^50 ^50 ^50 O o II II -s=o — s=o D**R -S=NR 117 * 115 1 N=0 Ri 14* R — P=D* 114* 114* and R 114 ** R 114* — P=D* ' , wherein D* and D** independently have the meaning of D as R-114** previously defmed; Rn 4*> R 114* *, R 115 and Rn 7 * have the meaning of R l4 *, Rι **, Rχ 5 and Rι 7* respectively, as previously defmed; R 50 and R 51 are as previously defined or R 50 and R51 together form part of a saturated or unsaturated cyclic, bicyclic or fused ring system as defined herein; R 2 * is selected from the group consisting of R 2 as previously defined, Px as previously defined, S(O) z OR 12 o and S(O) z NR 120 Rι 2 ι, wherein z is 1 or 2; R 33 and R 34 are independently selected from the group consisting of hydrogen and R 20 as previously defined, or R 33 and R 3 together form a saturated or unsamrated cyclic, bicyclic or fused ring system as defined herein, and R 120 and R 121 independently have the meamng of R 20 as previously defined, or R 120 and R 121 together form a samrated or unsamrated cyclic, bicyclic or fused ring system as defined herein, R 30 is as previously defmed, and Y** is selected from =N-NR 115 R 117 and =N-OR U5 , wherein R U5 and R 117 have the meaning of R 15 and R respectively, as previously defined, or Rns and R 117 together form a samrated or unsaturated cyclic, bicyclic or fused ring system as defined herein, and wherein any group selected from R ls Rj*, R 2 , R 2 *, R 9 , R π , R 12 , R 13 , R 50 and RSJ may, together with any other group selected from Rj, Rj * , R 2 , R 2* , R 9* , Rιo > Rn > R 12 , R 13 , R 50 and R 51 form one or more samrated or unsamrated cyclic, bicyclic or fused ring system(s) as defined herein, ^N-O and wherein any tertiary amino nitrogen atom may be replaced by the group and, wherein any hydroxyl, mercapto or amino group may be protected by a protecting group which is labile in vivo. 2. A compound according to claim 1, of the general formula (T) or a pharmaceutically acceptable salt or prodrug thereof: W-(A , ) n .-B'-(A , *) m .-V (T) wherein W is selected from the group consisting of R^-X-, R'^-X*-, -Y'*, -CN, -N=CR 5 R 5 *, -C(R 5 )=NR 3 , -C(R 5 )=NOR 3 , -C(D)OR 3 , -C(D)SR 3 and -C(D)NR 3 R 4 , wherein Y'* is as defined below, R 1 ; R 3 and R 4 are independently selected from the group consisting of R and a solubilising group Px which is labile in vivo, wherein R is selected from the group consisting of hydrogen, R 20 , wherein R 2Q is selected from the group consisting of optionally substituted (Cι-Cι 8 )alkyl, optionally substituted (C 2 -C 18 )alkenyl, optionally substituted (C 2 -C 1 )alkynyl, optionally substituted (C 3 -C 18 )cycloalkyl, optionally substituted (C 3 -C 18 )cycloalkyl(C 1 -Cι )alkyl, optionally substituted (C 3 -C 18 )cycloalkyl(C 2 -C 18 )alkenyl, optionally substimted (C 3 -C 18 )cycloalkyl(C 2 -Cι )alkynyl, optionally substituted (Cg-C 24 )aryl, optionally substimted (C 6 -C 24 )aryl(C 1 -C 18 )alkyl, optionally substimted (C 6 -C 24 )aryl(C 2 -C 18 )alkenyl, optionally substituted (C 6 -C 4 )aryl(C 2 -C 18 )alkynyl, optionally substituted (C r C 18 )acyl, optionally substituted heterocyclic, optionally substituted heterocyclic(C r C 18 )alkyl, optionally substituted heterocyclic(C 2 -C 18 )alkenyl, and optionally substituted heterocyclic(C 2 -C 18 )alkynyl C(D)OR 21 , C(D)SR 21 , and C(D)NR 21 R 22 , wherein R 21 and R 22 independently are selected from hydrogen and R 20 as previously defined, or R 21 and R 22 together form a saturated or unsaturated cyclic, bicyclic or fused ring system as defined herein, or R 3 and R 4 , when present, together torm a samrateα or unsamrated cyclic, bicyclic or fused ring system as defined herein, D is selected from O and S, X is selected from the group consisting of Y', S(O) and S(O) 2 wherein Y' is as defined below, X* is selected from the group consisting of NR 10 , O and S, wherein R 10 has the meaning of R as previously defmed, R' l * is selected from the group consisting of Ri as previously defmed, S(O) z OR 7 and S(O) z NR 7 R 8 , wherein z is 1 or 2 and R 7 and R 8 independently have the meaning of R 2Q as previously defined, or R 7 and R 8 together form a samrated or unsamrated cyclic, bicyclic or fused ring system as defmed herein, R 5 and R5* are independently selected from the group consisting of H, CF 3 , C(D)OR 103 , C(D)SR 103 C(D)NR 103 R 104 and R 20 as previously defined, wherein D is as previously defmed, and wherein R 103 and R lυ4 have the meaning of Rβ as previously defined, or R^ and R 10 together form a samrated or unsaturated cyclic, bicyclic or fused ring system as defined herein; n' is 0-8; m' is 0-8 and n' +m' > 1; A' and A'* are independently at each occurrence selected from the group consisting of O, S, S(O), S(O) 2 , NR n , CR 12 R 13 and CR 12 *R 13* , or two consecutive groups A' -A' or A'*-A'* are a structural unit selected from — C≡C — » wherein and R- 12 *» R l3 *> ^ 9 an( * R 9 * are independently selected from the group consisting of F, Cl, Br, I and R 5 as previously defined, Rn has the meaning of R ! as previosly defined, R^ 2 has the meaning of Rβ as previously defmed, R 13 is selected from the group consisting of F, Cl, Br, I, Rβ as previously defined, and R oo > wherein R 20 o is selected from the group consisting of CN, NCO, NCS, OCN, SCN, N 3 . OReo, SRόO' NRβoRόi. D 1 C(D 2 )R 60 , D 1 C(D 2 )D 3 R 60 , D 1 C(D 2 )NR 60 R 61 , NR 60 C(D 1 )R 61 , NR 60 C(D 1 )D 2 R 61 ) NR 60 C(D 1 )NR 61 R 62 , NRfioORβ!, amidino, guanidino, S(O)R6o, S(O) 2 D 1 R 60 , SCO NRβoRβi, P(D 1 )(D 2 R 60 )R 61 , P(D 1 )(D 2 R 60 )D 3 R 61 , P(D 1 )(D 2 R 60 )NR 61 R 62 , P(D 1 )R 60 R6i, D 1 P(D 2 )(D 3 R 60 )R 61 , D 1 P(D 2 )(D 3 R 60 )D 4 R 61 , D 1 P(D 2 )(D 3 R 60 )NR 61 R 62 , D 1 P(D 2 )R 60 R 6 ι, NR 60 NR 61 R 62 and ONRgoRόi, wherein O , D 2 , D 3 and D independently have the meaning of D as previously defmed, and and Rg 2 independently have the meaning of Rβ as previously defined or any two or more of R^ Q , ROI and Rβ 2 form part of a samrated or unsamrated cyclic, bicyclic or fused ring system as defined herein, and R 13 together are selected from the group consisting of =O, =S, =NOR 60 , =NR 60 , -OQO-, -SQS- and -SQO-, wherein Q is optionally substituted (CpC^alkylidene as defmed herein and R βQ is as previously defined; selected from the group consisting of Rl4* ZM Mi M 2 2 D* O — C — I I I II II II I — N — — N — — N— — C — — C — , — S— R14 OR-is ORi5 — C— — C— I and I SR-ig NR-|3*R-|9* wherein R2o 3 and R 2 o3* independently have the meaning of R as previously defined, R 1 * and R 14 ** are independently selected from the group consisting of hydrogen, R 2 n as previously defmed, CF 3 , C(D*)SR 40 and C(D*)NR 4Q R 4 I , wherein R 0 and R 1 independently have the meaning of R 21 and R 22 as previously defmed or R40 and R41 form part of a samrated or unsamrated cyclic, bicyclic or fused ring system as defmed herein, R 14 is selected from the group consisting of F, Cl, Br, I, R 14* as previously defined and R 2Q O as previously defined, R 17 and R 17 * independently have the meaning of R β as previously defined, D* has the meaning of D as previously defined, Z is a saturated or unsaturated (C 2 -C )alkylidene radical which is optionally substituted with one or more groups selected from F, Cl, Br, I and Rj 4 * as previously defined, Z* is a samrated or unsaturated (Cι-C 3 )alkylidene radical which is optionally substituted with one or more groups selected from F, Cl, Br, I and R^ * as previously defined, M i is selected from the group consisting of OR^, SR 15 and NRi5Rι 7 , wherein R^ is selected from the group consisting of: Px as previously defined, R β as previously defined, , , wherein Px and D are as previously defined and R is H or C 1 -C 4 alkyl, and a glycosyl radical which is derived from a synthetic or namrally occurring aldose, ketose, deoxyaldose, deoxyketose, aminoaldose, aminoketose or an oligosaccharide thereof, and Rι 7 is as previously defined, or R j5 and R 1 together form a saturated or unsaturated cyclic, bicyclic or fused ring system as defined herein, M and M* are independently selected from the group consisting of M^ as previously defmed, OCN, SCN, Y'R 2 , Y'* and N = CR 30 R 31 , wherein Y', Y'* and R 2 are as defmed below, and R 30 and R 31 independently have the meaning of R 20 as previously defined, M 2 is selected from the group consisting of R 1 * as previously defmed, where Y** is as defmed below, R 30* has the meaning of R 2Q as previously defined, and R j7* is as previously defmed, R 18 and R^ independently have the meaning of R 20 as previously defined or R 1 and R 19 together form part of a samrated or unsamrated cyclic, bicyclic or fused ring system as defined herein, and R 18 * and R 19 * together form part of a samrated or unsamrated cyclic, bicyclic or fused ring system as defined herein; selected from the group consisting of Y'R 2 , Y'* and C(R 30 )=Y**, wherein Y' is selected from the group consisting of o 0- O " II I — S— N— -N=N- — N=N- — N=N- I + + R50 o o o -S-N— — N-S— — N-S — _o_ S — II I I I II n O R 50 R50 R50O o o o o o II II — s-o — — s— s — -o— s — — s-o- II II o o o o o — S-S— — S-S— — P-N— — O-P-N— II I I I ' O 51O R50 51O 50 0 0 0 o II II II — N— P — — N— P-O— — P— O— — O Λ — J Pl — I I I I I I R50OR51 R50OR51 0R 51 0R 51 5 > 5 ' O O o o II II II II — P— N — — N— P — — P— O— — O— P — I I I I I I and R51O R50 R50OR51 R52 R52 O II — o— p -o- I OR51 wherein R 50 has the meaning of R as previously defmed, R 51 has the meaning of R $ as previously defined and R 5 has the meaning of R 2 o as previously defmed, or R 50 and R 51 together form part of a samrated or unsamrated cyclic, bicyclic or fused ring system as defined herein, and R 2 has the meaning of Rβ as previously defined, Y'* is selected from the group consisting of R 33 — N— N-R 2 * — N-N=C — N-0-R 2 * — O— N-R 2 * I I I V R I ^ I z R50 R51 R50 M R50 R50 R114* — P=D* 1 , wherein D* and D** independently have the meaning of D as R114** previously defined; Rn 4* » R 114 **, R 115 and Rn 7* have the meaning of R 14 *, R 14 **, R 15 and R 17 * respectively, as previously defined; R 50 and R 51 are as previously defined or R 50 and R 51 together form part of a samrated or unsaturated cyclic, bicyclic or fused ring system as defined herein; R 2 * is selected from the group consisting of R 2 as previously defined, S(O) z OR 1 o and S(O) z NRι 2 oRι 2 ι, wherein z is 1 or 2; R 33 and R 34 are independently selected from the group consisting of hydrogen and R 2 o as previously defined, or R 33 and R 34 together form a saturated or unsaturated cyclic, bicyclic or fused ring system as defmed herein, and R 12Q and R 121 independently have the meaning of R 2Q as previously defined, or RJ 2Q and R 121 together form a samrated or unsamrated cyclic, bicyclic or fused ring system as defined herein, R 30 is as previously defmed, and Y** is selected from =N-NRn 5 Rn 7 and =N-OR 115 , wherein R n s and R 117 have the meaning of R 15 and R respectively, as previously defined, or Rns and R 117 together form a saturated or unsamrated cyclic, bicyclic or fused ring system as defined herein, and wherein any group selected from Rj, R *_ R 2 , R 2* , R 9 , Rn, R 12 , R 50 and R 51 may, together with any other group selected from R ls R^*, R 2 , R 2 *, R 9 *, R^, Rn, Rι 2 , R 50 and R 51 form one or more saturated or unsamrated cyclic, bicyclic or fused ring system(s) as defmed herein, ^N-0 and wherein any tertiary amino nitrogen atom may be replaced by the group , and, where the sequence W'-(A') n .-B , -(A , *) m .-V , contains a grouping of three heteroatoms together, one atom of those three heteroatoms is oxidised sulfur in the form of S(O) or S(O) 2 , or oxidised phosphorus in the form of P(O), or the three heteroatoms comprise two nitrogen atoms which form part of a heterocycle, provided that the sequence W , -(A , ) n -B'-(A'*) m .-V' does not contain two oxygen atoms together or three sulfur atoms together; and wherein (a) when W is R'χ*X* wherein X* is NR 10 , and V is Y'* wherein Y'* is — N— N-R 2 * O R 80 o R5θ Rδ1 , and B' is ~ ~ ? _ or — C ~ δi wherein R ι is selected from the group consisting of hydrogen, -RJOOH, -R 100 C(O)OR 10 ι, -RιooC(O)NR 10 ιRιo 2 , -R 100 _NR 102 C(0)R 10 o* and - R 100 C (°) R 100*' wherein R^i and Rκ) 2 are independently selected from the group consisting of hydrogen, optionally substituted optionally substituted (C 3 -C 1 g)cycloalkyl, optionally substituted (C 3 -C 18 )cycloalkyl-(C 1 -C 18 )alkyl, optionally substituted (C 6 -C 2 4)aryl, optionally substituted (C 7 -C 2 5)aralkyl, optionally substituted (C 2 -C 18 )alkenyl, optionally substituted (C 8 -C 26 )-aralkenyl, optionally substimted (C 2 -C 18 )-alkynyl, optionally substimted (C 8 -C 26 )- aralkynyl and optionally substituted heterocyclic, and wherein R^O Q and RI Q O* are independently divalent radicals derived from a member selected from the group consisting of (Cι-Cιg)alkyl, (C 3 -C 18 )cycloalkyl, (C 3 -C 18 )cycloalkyl(C 1 -C 18 )alkyl, (C 6 -C 24 )aryl, (C 7 -C 25 )aralkyl, (C 2 -C 18 )alkenyl, (C 8 -C 26 )aralkenyl, (C 2 -C 18 )- alkynyl, (C 8 -C 26 )aralkynyl and heterocyclic, any of which may be optionally substimted as defined herein, and R o is selected from the group consisting of R 81 as previously defined and a solubilising and/or protecting group Px which is labile in vivo, then at least one of the following applies: (i) R 50 is a group R 53 , wherein R 53 is selected from the group consisting of C(D*)OR 21 *, C(D*)NR 21 *R 22 *, C(D*)SR 21 *, C(D*)R 55 , CF 3 , R 55 and a solubilising group Px which is labile in vivo, wherein D* has the meaning of D as previously defined, R 21 * and R 22 * have the meamng of R 2 ^ and R 22 respectively, as previously defined, and wherein R 55 is selected from the group consisting of optionally substimted (C 1 -C 18 )alkyl(C 6 -C 24 )aryl, optionally substituted (C 2 -C 18 )alkenyl(C 6 -C 2 )aryl, optionally substimted (C 2 -C 18 )- alkynyl(C 6 -C 2 )aryl, optionally substituted (C 3 -C 18 )cycloalkyl- (C 2 .C 18 )alkenyl, optionally substituted (C 3 -C 18 )cyclo- alkyl(C -C 18 )alkynyl, optionally substituted (C 3 -Cι 8 )cycloalkyl- (C 6 -C 24 )aryl, optionally substituted acyl(C 6 -C 24 )aryl, optionally substituted heterocyclic^ ! -C 18 )alkyl, optionally substimted hetero- cyclic(C 2 -Cι 8 )alkenyl, optionally substituted heterocyclic- (C 2 -C 18 )alkynyl and optionally substituted heterocyclic(C 2 -C 18 )- (C 6 -C 24 )aryl, and n', m', R'ι*, RJQ, A', A 1 *, R 51 and R * are as previously defined, (ii) one of R 2 * and R 51 is a group R 54 , wherein R 54 is selected from the group consisting of R 55 *, C(D*)NR 21 *R 22 *, C(D*)OR 55 *, C(D*)R 55 *, C(D*)SR 21 *, CF 3 , S(O) Z OR 120 , S(O) Z NR 120 R 121 , and a solubilising group Px which is labile in vivo, wherein z is 1 or 2 and R 12 Q and Rj 2 ι are as previously defmed or R 1 2 0 and R 121 together form a saturated or unsamrated cyclic, bicyclic or fused ring system as defined herein, and wherein R 2 χ* and R 2 * have the meaning of R 21 and R 22 respectively, as previously defmed, and R 55* has the meamng of R 55 , as previously defined, and n', m', R' , R^, A', A'*, R 50 and the other of R 2* and R 5J are as previously defined, (iii) at least one A' or A 1 * is selected from the group consisting of CR 112 R 13 , CRι 2 Rn 3 > CRn 2 R i 3 * and CR 12 *Rn 3 » wherein Rn 2 and R 113 are independently selected from the group consisting of R 55 as previously defined, C(D)OR 21 *, C(D)SR 21 *, C(D)NR 21 *R 22 *, F, Cl, Br and I, wherein R 21 * and R 2 * have the meaning of R 21 and R 22 respectively, as previously defined, and D, n', m', R' j*, R 2* , Rιo> Rn, i 2 > Ri 2 *> Ri 3 > Ri 3 *> R 50 and R 51 are as previously defined, (iv) R'ι * is selected from the group consisting of optionally substimted (C -C 18 )alkenyl, optionally substimted (C 2 -C 18 )alkynyl, optionally substimted (C 3 -C 18 )cycloalkyl(C 2 -C 18 )alkenyl, optionally substituted (C 3 -C 18 )cycloalkyl(C -C 18 )alkynyl, optionally substimted (C 6 -C 2 )aryl- (C 2 -C 18 )alkenyl, optionally substimted (C 6 -C 2 )aryl(C -C 18 )alkynyl, optionally substituted (C 2 -C 18 )acyl, wherein the optional substi ent is other than amino, optionally substituted (C 6 .C 24 )aryl(C 2 -C 18 )acyl, optionally substimted heterocyclic(C 1 .C 18 )alkyl, optionally substimted heterocyclic(C 2 -C 18 )alkenyl, optionally substituted heterocyclic(C 2 -C 18 )alkynyl, C(O)OR 90 , C(O)NR 91 R 92 , CF 3 , S(O) Z OR 120 , S(O) z NR 120 Rι 2 ι and a solubilising group Px which is labile in vivo, wherein z is 1 or 2 and R 120 and R 121 are as previously defined, wherein R 90 is selected from the group consisting of (C 3 -C 18 )cycloalkyl, (C 3 -C 18 )cycloalkyl(C r C 18 )alkyl, heterocyclic, (C r C 18 )alkyl- heterocyclic, (C 6 -C 24 )aryl, (C 6 -C 24 )aryι^ 1 - , 18 aικy auu (C 6 -C 24 )aryl(C i -C 8 )alkylheterocyclic , and wherein R 91 and R 92 are independently selected from the group consisting of optionally substimted (C 2 -C 18 )alkenyl, optionally substituted (C 2 -Cι )alkynyl, optionally substimted (C 3 -Cι )cycloalkyl, optionally substimted (C 3 -Cι 8 )cycloalkyl- (C 1 -Cχ 8 )alkyl, optionally substimted (C 3 -C 1 )cycloalkyl- (C 2 -Cιg)alkenyl, optionally substituted (C 3 -C 8 )cycloalkyl- (C -Cχg)alkynyl, optionally substimted (C 6 -C 24 )aryl- (C 2 -C 1 g)alkenyl, optionally substituted (C 6 -C 2 )aryl- (C 2 -Cιg)alkynyl, optionally substimted (C 2 -Cι 8 )acyl, optionally substituted (C 6 -C 2 4)aryl(C 2 -C 18 )acyl, optionally substituted heterocyclic, optionally substituted heterocyclic(C 1 -C 18 )alkyl, optionally substituted heterocyclic(C 2 -C 18 )alkenyl, and optionally substimted heterocyclic(C .C 18 )alkynyl, or R 91 and R 92 together form a samrated or unsamrated cyclic, bicyclic or fused ring system as defined herein, and m\ n', A', A'*, R 2 *, R 50 , R 51 and R 10 are as previously defined, (v) a group selected from R l5 R'j*, R 2 , R 2 *, R 9 , Rn, Ri 2 ' R 50 and R 5l > taken together with another group selected from R l 5 R' ι*, R , R 2 *, R 9 *, Rio, n» Ri 2> R 50 and R 51 is selected from the group consisting of -C(O)- and optionally substituted methylene; (b) when W is R *X* wherein X* is NR 10 , and V is Y'* wherein Y'* is — N— N-R 2 * I I 50 51 , and B' is selected from -CH(OH)- and -C(O)- then at least one of the following also applies when one of the conditions (i) to (iv) defined above in (a) applies: (vi) n' > 1, (vii) n' = 0, (viii) m' > 1, (ix) m' = 0, (x) R 50 and R 51 together form part of a saturated or unsamrated cyclic, bicyclic or fused ring system as defined herein, (xi) R 50 is a group R 5 β, wherein R 56 is selected from the group consisting of C(D*)OR 2 ι * , C(D*)NR 2 ι * R 22* , C(D*)SR 2 ι * , C(D*)R 55 and a solubilising and/or protecting group Px which is labile in vivo, wherein R 2 ι * and R 22* are as previously defined, and (xii) n' = m' = 1 and A'* is other than -CH 2 -, R-14* R-I7 R14* and (c) when B' is selected from — p — -O— — S— -N— — N — Rl4* — C— I and 14 , wherein Rι 4 , Rι 4 * and R 7 are as previously defined, then at least one group selected from R 2 or R 2 *, Rn, R i2 , R 50 and R 51 together with another group selected from R l s or Ri*, R 0 , Rn and Rχ 2 forms a saturated or unsaturated cyclic, bicyclic or fused ring system as defined herein, said ring being substimted with at least one polar group selected from =O, =S, OH, SH, NHR 10 * and C(O)OH, wherein Rι 0 * has the meaning of R O as previously defined, said polar group being sterically capable of being located within the compound of formula (I) not more than 5 Angstrom units from the P, O, S, N or C atom of group B, provided that when W is R' 1+ X* and X* is NH and V is Y'* wherein Y'* is wherein R' * is other than H and R 71 and R 72 are independently selected from the group consisting of H, (C -Cg)alkyl, optionally substituted phenyl, optionally substimted naphthyl, optionally substituted phenyl(C -C 2 )alkyl and optionally substimted naphthyl- (Cι~C 2 )alkyl, and when (a) B' is -CH(OH)- and (A') n is -CH(R 73 )- wherein R 73 is selected from the group consisting of (Cι-C 6 )alkyl optionally substimted with 1-5 fluorine atoms, (C 3 -C 6 )alkenyl, (C r C 6 )alkoxy-CH 2 -, (CH 2 ) p phenyl, (CH 2 ) p naphthyl, (CH 2 ) p (C 5 -C 6 )cycloalkyl and (CH 2 ) p indolyl, wherein said (CH 2 ) n phenyl, (CH 2 ) n naphthyl, (CH 2 ) n (C 5 -C 6 )cycloalkyl and (CH 2 ) n indolyl are optionally substituted with nitro, halogen, (C -C^alkyl, (C r C 4 )alkoxy or (Cι-C 4 )alkylthio and wherein p is 0, 1 or 2, then (A'*) m . is other than OHO — CH 2 -c-c- wherein R 74 has the meaning of R 73 as previously defined, and R when OH (b) B' is —C— wherein R 74 has the meaning of R 73 as previously defined and R74 H H I I I (A') n - i c-c-c I I I wherein R 73 is as previously defmed, then (A'*) m - is R 73 0H H other than -C(O)-, and when H H H H I I I I (c) B' is -C(O)- and (A') n - is — C-c-C-C- wherein R 73 is as previously R 73 OH H OH defined, then m 1 is other than 0. 3. A compound according to claim 1, wherein B is selected from the group consisting of M ZM M 2 I i I ZM Mi M 2 P * ~~ ? — — C— - " _ I I I II I I I — N — — N — — N — — C — , Ri4* R 14 Ri4 where Z, Z*, M, M j , M 2 , D*, R i4 , R 14* , R M **, Rι 5 , Rι 8 , R i8* , R i9 and R 19 * are as defined in claim 1 , V is YR 2 , Y* or C(R 30 )=Y**, wherein R 2 , R 30 and Y** are as defined in claim 1, Y is 0 " o- _ _ l l _ _ selected from the group consisting of N , N—N ^ N—N ? an ^ / R33 — N-N-R 2 * -N-N=C I I I R34 Y* is selected from the group consisting of R50 R51 R50 — N— O— R 2 * — O— N— R 2 * R R 50 and , wherein R 33 , R 3 , R 50 , R 51 and R 2 * are as defined in claim 1. 4. A compound according to claim 1 having the strucmre represented by formula (IA): wherein Ri * , RJQ, R 12 , Ri 2*> R l3 and R i3* are as defined in claim 1, B* is selected from the group consisting of where Z, Z*, M, Mj, M 2 , D*, R J4 , R 14* , R 14 **, Rι 8 and R 19 are as defined in claim 1, and Y l is selected from the group consisting of — N— N-R 2 * — N-0-R 2 * — O— N-R 2 * I I I I R5 ° Rδ1 , Rδ0 and Rδ0 wherein R 50 , R 51 and R 2 * are as defined in claim 1. 5. A compound according to claim 1 of the general formula (IB): wherein x and y are independently 0 or 1 , B is selected from the group consisting of wherein Rι 4* , Rι 4 **, R 15 , Rι 8 and R 19 are as defined in claim 1 and each R 560 is independently hydrogen or (Cι-C 4 )alkyl, R 502 and R 506 are independently a group Rgoo, wherein Rgoo is selected from the group consisting of hydrogen, C(O)OR 62 ι, C(O)SR 62 ι, C(O)NR 62 ιR 622 , (C r C 6 )alkyl, (C 2 -C 6 )alkenyl, (C 5 -C 10 )cycloalkyl, (C 5 -C 10 )cycloalkyl(C C 6 )alkyl, (C 5 -C 10 )cycloalkyl(C 2 -C 6 )alkenyl, (C 6 -C 10 )aryl, (C 6 -Cι 0 )aryl- (C r C 6 )alkyl, (C 6 -Cι 0 )aryl(C 2 -C 6 )alkenyl, (C r C 6 )acyl, heterocyclic, heterocyclic(C r C 6 )alkyl and heterocyclic(C 2 -C 6 )alkenyl, each of which may be substimted by up to three substiments selected from the substituents defined herein for "optionally substimted (C r C 18 )alkyl" and R^i and R^ have the meaning of R 21 and R 22 respectively, as defmed in claim 1, or Rg 2 ι and R 622 together form a samrated or unsaturated cyclic, bicyclic or fused ring system as defined below, R 50 ι is selected from the group consisting of Rgoo as previously defined, S(O)ORg 32 , S(O) 2 R 632 , S(O)NR 632 R 633 , S^R^R^, NH 2 , NHRg 3 ι and NR_ 63 ιR 632 , wherein R 3 has the meaning of Rg as defined in claim 1 and Rg 32 and Rg 33 independently have the meaning of R 20 as defined in claim 1, or R5 01 and R 506 together form part of a saturated or unsamrated cyclic, bicyclic or fused ring system, or Rg 31 and Rg 32 , or Rg 32 and Rg 33 together form a saturated or unsamrated cyclic, bicyclic or fused ring system as defined herein, R 5 ι 2 and R 5 2 independently have the meaning of R 600 as previously defined, R5 22 and R 532 are independently selected from the group consisting of R oo as previously defmed, F, Cl, Br and I, R 5l3 and R 54 are independently selected from the group consisting of Rgoo as previously defined and R 20 o as defined in claim 1, R 523 and R 533 are independently selected from the group consisting of Rgoo as previously defined, F, Cl, Br, I, and R 20 o as defined in claim 1, R 550 has the meaning of Rβ as defined in claim 1 and R 55 ι is selected from the group consisting of R 50 , hydrogen, S(O)OR 632 , S(O) 2 Rg 32 , S(O)NR 632 R 633 and S(O) 2 Rg 32 Rg 33 , wherein Rg 50 has the meaning of Rg as defined in claim 1 and Rg 32 and Rg 33 are as previously defmed, or Rg 32 and Rg 33 together form a samrated or unsaturated cyclic, bicyclic or fused ring system as defined herein, or R5 50 and one of R 55 and RSQ 2 together form a diazaheterocycle wherein R 550 , R 551 or RSQ 2 and the two nitrogen atoms to which they are bonded are part of a stable 5 to 10-membered ring which may comprise up to two further heteroatoms selected from O, S and N and to which may be fused one or more cycloalkyl, cycloalkenyl, aryl or heterocyclic residues, which diazaheterocycle may be substimted by one or more of the substiments defmed herein for "optionally substimted (Cι-Cι )alkyl", and wherein two substiments may together form part of a ring, or one pair selected from Rsι 2 and Rsι 3 , Rs 22 and R 523 (when present), Rs 32 and R 533 (when present), and R 5 2 and Rs 43 , together are =O; O 0 R 15 wherein, when B is other than J! or — C — then at least one of conditions I R-I4* (i) to (xi) below applies: (i) at least one of Rsι 2 and R 542 is a group Rg 55 , wherein Rg 55 is selected from the group consisting of (C r C 6 )alkyl(C 6 -Cιo)aryl, (C 2 -C 6 )alkenyl(C 6 -Cι 0 )aryl, (C 5 -C 10 )cycloalkyl(C 2 -C 6 )alkenyl, (C 5 -Cι 0 )cycloalkyl(C 6 -C 10 )aryl, acyl(C 6 - ια >aryl, heterocyclic(C -Cg)alkyl, heterocyclic(C 2 - 6 )alKenyl, heterocychc- (C 6 -C 10 )aryl, C(D*)OR 2 ι * , C(D*)SR 2 ι * and C(D*)NR 2 ι * R 22* , wherein D*, R 2l * and R 22 * are as defined in claim 1, (ii) at least one of Rs 22 and Rs 32 , when present, is selected from the group consisting of Rg 55 as previously defined, F, Cl, Br and I, (iii) at least one of R5 3 and Rs 3 , when present, is selected from the group consisting of Rg 55 as previously defined, and R 0Q as defined in claim 1 , (iv) at least one of Rs 3 and Rs 33 , when present, is selected from the group consisting of Rg 55 as previously defined, F,C1 Br, I and R 2 oo as defined in claim 1, (v) R 55 o is a group Rgsg, wherein Rg 5 g is selected from the group consisting of (C 1 -C 6 )alkyl(Cg-C 10 )aryl, (C 2 -C 6 )alkenyl(C 6 -C 10 )aryl, (C 5 -C 10 )cycloalkyl- (C 2 -C 6 )alkenyl, (C 5 -C 10 )cycloalkyl(C 6 -C 10 )aryl, acyl(C 6 -Cι 0 )aryl, heterocyclic(Cι-C 6 )alkyl, heterocyclic(C 2 -C 6 )alkenyl, heterocyclic- (Cg-C 10 )aryl, (vi) R 551 is selected from the group consisting of Rg 5 g as previously defmed, S(O)ORg 32 , S(O) 2 Rg 32) S(O)NRg 32 Rg 33 and S(O) 2 R 632 Rg 33 , wherein Rg 32 and Rg 33 are as previously defined, (vii) R 50 is selected from the group consisting of Rg5g as previously defined, C(D*)SR 2 ι* and C(D*)NR 21 *R 22 *, wherein D*, R 2J * and R 22 * are as defined in claim 1, (viii) R 502 and R 55 ι are both hydrogen or are both (Cι-Cg)acyl, (ix) R 14 * is selected from the group consisting of C(D*)OR 0 , C(D*)SR 40 and C(D*)NR 0 R ι, wherein R 40 and R 41 are as previously defmed, (x) R 501 is selected from the group consisting of Rg 5 g as previously defmed, S(O)ORg 32 , S(O) 2 Rg 32 , S(O)NRg 32 Rg 33 , S(O) 2 Rg 32 Rg 33 , NH 2 , NHRg 3 ι and NRg 3 ιRg 32 , wherein Rg 32 and Rg 33 are as previously defined, (xi) R 50 ι and R 50 g are both (C -Cg)acyl, OH and wherein when B is -C | - or ° I then at least one of the following H ϋ conditions also applies: (xii) x + y > 0, (xiii) x + y = 0 and at least one of R 532 and R 533 is other than hydrogen, (xiv) R 50 and R 51 together form a diazaheterocycle as previously defined, (xv) at least one of R 501 , Rso 2 > R 5O6 an d R 551 is optionally substimted heterocyclic(Cι-Cι 8 )alkyl, and (xvi) at least one of R 512 , R 542 , R 522 , R 532 , R 5 ι 3 , R 543 , R 523 and R 533 is selected from the group consisting of C(O)ORg 2 ι, C(O)SRg 2i and C(O)NRg 2 Rg 22 , wherein Rg 2 ι and Rg 22 are as previously defmed. A compound according to claim 1 comprising at least one solubilising group Px, wherein Px is selected from the group consisting of Px*, wherein D is O or S, R is H or C r C alkyl, and wherein Px* is selected from: or, wherein the compound of formula (I) as defined in claim 1 includes two functional groups capable of being derivatised by a solubilising group Px, said two functional groups being in sufficiently close proximity to one another, comprising a cyclic strucmre including a structural unit selected from: wherein Xi and X are independently selected from O, S and NRg wherein Rg is as defined in claim 1. 7. A compound according to claim 6 wherein said solubilising group is selected from O O II II ^P-OH ^P-OH 0H and H . 8. A compound according to claim 1, selected from the group consisting of formula (IC) to (IAW), wherein each AA is independently a residue of a namrally occurring or synthetic amino acid as herein defined; Ri*, Rj, X and X* are as defined in claim 1; R a to Rj independently are -(CH 2 ) a .gOPy or Rg, wherein a can be 0, 1, 2, 3, 4 or 5, and wherein Py is a solubilising group Px as defined herein, and Rg is as defined in claim 1 : wherein D' is O or S, and each G is independently hydrogen or R 20 o as defined in claim 1 and wherein R'^ and R' f are R^ and R or, taken together, may be trimethylene or tetramethylene optimally substituted with -C(O)OR; or -C(O)NRiR j ; wherein G is selected from Ri * and X*Rι * ; wherein R a ' is OPy or Rg as defined in claim 1, Mi is Rg as defined in claim 1, (CH 2 )ι_ 2 OPy or (CH 2 )ι_ 2 NHPy, and G* is OR 2 or NRjR 2 ; wherein G is hydrogen, R a , Rι*X* or Rι*X*C(R a )(R b )C(O), and wherein R a , R *, and the atoms to which they are bound may optionally form a samrated or unsamrated cyclic, bicyclic or fused ring system; wherein R a , Rj*, and the atoms to which they are bound may optionally form a saturated or unsamrated cyclic, bicyclic or fused ring system; (ID wherein W2 is R X or Rg as defined in claim 1, and R' is Py or Rg as defmed in claim 1, or R' and Py, taken together with the oxygen atoms to which they are attached form a HO H O o o group selected from . , ,?^ and ,s / 6 -o 0- -o 0- -o 0- wherein each L is independently as defined in claim 1 and each Pz is independently hydrogen or Py, provided that at least one Pz is Py or, when each Pz is Py, the groups Py, together with the oxygen atoms to which the are bound define a cyclic group selected HO p H p o_ p from _ , ^ and .s ; -o o- -o o- -o o- wherein Q is O or NR f and G is Ri* or X*R t* ; wherein each NHet) is independently a 5- or 6- membered samrated or unsamrated heterocycle containing a nitrogen atom and optionally additionally one or two heteroatoms selected from nitrogen, oxygen and sulfur, and wherein R a ' and R b ' independently have the meaning of -(CH 2 )o- 6 θPy or R θ > or taken together are = O; . wherein Wi is selected from RiX and Rι * X*, and Q is selected from O and NR h ; wherein Wi is selected from RiX and R *X*, each Pz is independently hydrogen or Py, provided that at least one Pz is Py, and Q is selected from O and NR b ; wherein each Pz is independently hydrogen or Py, provided that at least one Pz is Py; wherein NHet) is a 5- or 6- membered samrated or unsamrated heterocycle containing a nitrogen atom and optionally additionally one or two heteroatoms selected from nitrogen, oxygen and sulfur; wherein R a ' and R j ' are independently selected from Rj and Ri * , as defined in claim 1; Re Re Rα i \ r wherein G is selected from — C — ' — C— C — and a saturated or unsaturated I I I Rf Rf Rh cyclic, bicyclic or fused ring system, Q is O or NH, and G* is X or X* as defined in claim 1; wherein NHet) is a 5-12 membered samrated or unsaturated cyclic, bicyclic or fused ring system containing a nitrogen atom and optionally additionally from 1 to 4 heteroatoms selected from nitrogen, oxygen and sulfur; wherein G is selected from hydrogen and Rι*X*, Q is O, S or NH, Q* is O or NH, and G is selected from Ri and Rι*X*; wherein R 2QQ is as defined in claim 1 ; wherein NHet) is an optionally substituted 5-12 membered samrated or unsamrated cyclic, bicyclic or fused ring system containing a nitrogen atom and optionally additionally from 1 to 4 heteroatoms selected from mtrogen, oxygen and sulfur; wherein b is 0, 1 or 2, provided that at least one b is greater than 0, and each Pz is independently hydrogen or Py, provided that at least one Pz is Py; wherein each G* is independently selected from O, S and NRg and G is selected from ORg, NHRg and R 20 ; wherein G is -C(O)- or -CH 2 -, G* is Ri or R^, G ** is -O- or -NR h -, Q is -O- or -NRj and Pz is selected from the group consisting of OH wherein R and R' are independently hydrogen or C -C alkyl, D is O or S and Px* is as defined herein; wherein G is Ri or Ri*, G* is -O- or -NR f - and Pz is selected from the group consisting .Px* wherein R and R' are independently hydrogen or C r C alkyl, D is O or S and Px* is as defmed herein; wherein G is R } or Ri * , and each Q is independently H, -OPz or -NR d Pz, wherein each P z is independently hydrogen or Py, provided that at least one Pz is Py; wherein N Het J is a samrated or unsamrated cyclic, bicyclic or fused nitrogen containing ring system and G is a bond or is -O- or -NR f ; wherein G is absent or X*Rι* and Het is a 3 to 10-membered saturated or unsaturated heterocycle containing a nitrogen atom and optionally additionally one to three hetero¬ atoms selected from nitrogen, oxygen and sulfur; wherein Q is selected from -O-, -S- and -NR^; OPy wherein G is O, S, S(O) or S(O) 2 , and R a ' and R b ' have the meaning of R a and R b or R a > and R b - together are trimethylene or tetramethylene; wherein each Ar is independently (C 6 -Cι )aryl, R' c and R' are R c and R d or, taken together, are -C(O)- or -CH(OH)-, and wherein Pz and Pz' are independently hydrogen or Py with the proviso that at least one of Pz and Pz' is Py, or Pz and Pz' together with the HO^O H ^ O oxygen atoms to which they are attached form a group selected from -o' N o- -o' N o- and -o Λ o- wherein G is a bond or X as defined in claim 1, R g ' and R h ' are R g and R h or together form a samrated or unsaturated cylic, bicylic or fused ring system, and Pz and Pz' are independently hydrogen or Py with the proviso that at least one of Pz and Pz' is Py, or Pz and Pz' together with the oxygen atoms to which they are attached form a group selected from -o' o- -C o- and -o Λ o- . wherein G is a bond, O, S or NRj, R g ' and R h ' are R g and R h , or taken together may be - C(O)-, and Pz and Pz' are independently hydrogen or Py with the proviso that at least one of Pz and Pz' is Py, or Pz and Pz' together with the oxygen atoms to which they are H0 ^° attached form a group selected from -o' s o- -o' o- and -o o- OPs. wherein G is OPy, NHRg, NPyRg or 1^; wherein G and G* are independently a bond, O, S or NH, and R' d and R h ' are Rd and R h or taken together are -CR' - or -CR 2 '-CR 2 '- wherein each R' independently has the meaning of Rg as defined in claim 1, Q and Q* are independently N or CRg, or when Q* is CRg then R g and Rg together may be a double bond; wherein G is -C(O)- or -C(Rg)(CH 2 ) 0 ^OG* wherein G* is Rg or Py; wherein G is selected from hydrogen and X*Rι* and wherein I ) represents a 4-10 membered samrated or unsamrated cyclic, bicylic or fused ring system as defined herein; wherein Q is selected from O, S and NR g , G and G* are independently selected from R j , Ri*, -C(R 5 )=NR 3 and -C(R 5 )=NOR 3 , wherein R 3 and R 5 are as defined in claim 1, R' e and R'f are Rg and R f , and G** is R 20 as defined in claim 1; wherein each R z is independently selected from Rj and PyOG* wherein G* is optionally substimted alkylelne, provided that at least one R z is PyOG*, and G is -NRd- or CR^Re-; wherein ' — " represents an optionally substimted samrated or unsamrated ring system optionally containing up to three heteroatoms selected from N, O and S, G is selected from R l 5 XRi or X*Rι* and R a and R b taken together may optionally be -C(O)-; wherein B* is a group B, as previously defeined, derivatised with a solubilising group Py; wherein represents an optionally substituted cyclic, bicyclic or fused ring system containing a nitrogen atom and optionally additionally from 1 to 3 heteroatoms selected from N, O and S; wherein Qi and Q 2 are independently selected from O and S, and R' f and R' g are respectively R f and R g or are selected from OR', SR' and NR b R' wherein R' is H, R j or Py; wherein each G is independently selected from O and NR j , and R' is (CH 2 ) - 2 OPy or Rg; OQ OQOQ — C — — C-C— I I I wherein G and G* are independently selected from ^ , Re Rf and L, wherein L is as defined in claim 1 and Q is H or Py, provided that at least one of G and G* is other than L and provided that at least one Q is Py, or wherein two groups OQ taken together HO, JO R O o. JO / s / \ / are a cyclic group sleeted from ° ~ , ~ ° ° _ and ~ ° 0_ ; wherein R x and R y are independently Rg or (CH 2 )ι__ 2 OPy; wherein G and G* are independently selected from R l s Ri * , -C(R 5 )=NR 3 and -C(R 5 )N=OR 3 , wherein R 3 and R 5 are as defined in claim 1. 9. A compound according to claim 1 selected from the group consisting of (i) t-butyl 3-isopropyl-3-[(2R or S,3S)-2-hydroxy-3-(phenylmethoxycarbonyl)- amino-4-phenylbutyl]carbazate, (ii) t-butyl 3-isopropyl-3-[(2R or S,3S)-2-hydroxy-3-(N-quinaldoyl-L- valyl)amino-4-pheny lbutyl] carbazate , (iii) t-butyl 3-isopropyl-3-[(2R or S,3S)-2-hydroxy-3-(N-quinaldoyl-L- asparaginy l)amino-4-pheny lbutyl] carbazate , (iv) t-butyl 3-(l-methyl-3-phenylpropen-3-yl)-3-[(2R or S,3S)-2-hydroxy-3- (phenylmethoxycarbonyl)amino-4-pheny lbutyl] carbazate , (v) t-butyl 3-(l-methyl-3-phenylpropyl)-3-[(2R or S,3S)-2-hydroxy-3-(N- quinaldoyl-L-asparaginy l)amino-4-pheny lbutyl] carbazate , (vi) cis-1, 6-3-t-butoxycarbonyl-4-[(2R or S,3S)-2-hydroxy-3-amino-4- phenylbutyl]-3,4-diazabicyclo[4.4.0]decane, (vii) cis-1, 6-3-t-butoxycarbonyl-4-[(2R or S,3S)-2-hydroxy-3-(phenylmethoxy- carbony l)amino-4-pheny lbutyl] -diazabicyclo [4.4.0] decane , (viii) cis-1, 6-3-t-butoxycarbonyl-4-[(2R or S,3S)-2-hydroxy-3-(N-quinaldoyl-L- valy l)amino-4-pheny lbutyl] -3 ,4-diazabicyclo [4.4.0] decane (ix) cis-1 ,6-3-t-butoxycarbonyl-4-[(2R or S,3S)-2-hydroxy-3-[N-(2-pyridyl)- methoxycarbony 1)-L- valy l)amino-4-pheny lbutyl] -3 ,4-diaza-bicyclo [4.4.0]- decane (x) cis-1, 6-3-t-butoxycarbonyl-4-[(2R or S,3S)-2-hydroxy-3-(N-quinaldoyl-L- asparaginy l)amino-4-phenylbutyl]-3 ,4-diazabicyclo [4.4.0]decane , (xi) cis-1, 6-3-t-butoxycarbonyl-4-[(2R or S,3S)-2-hydroxy-3-(N-quinaldoyl-L- glutaminy l)amino-4-pheny lbutyl] -3 ,4-diazabicyclo [4.4.0] decane , (xii) cis-1, 6-3-t-butoxycarbonyl-4-[(2R or S,3S)-2-hydroxy-3-(N-quinaldoyl-L- threony l)amino-4-pheny lbutyl] -3 ,4-diazabicy clo [4.4.0] decane , (xiii) 2-t-butoxycarbonyl-3-[(2R or S,3S)-2-hydroxy-3-(phenylmethoxycarbonyl)- amino-4-phenylbutyl]-2,3-diazabicyclo[2.2.1]hept-5-ene, (xiv) 2-t-butoxycarbonyl-3-[(2R or S,3S)-2-hydroxy-3-(phenylmethoxycarbonyl)- amino-4-pheny lbutyl] -2 , 3-diaza-bicyclo [2.2.1] heptane , (xv) 2-t-butoxycarbonyl-3-[(2R or S,3S)-2-hydroxy-3-(N-(2-pyridyl)methoxy-L- valyl)amino-4-phenylbutyl]-2,3-diaza-bicyclo[2.2. l]heptane, (xvi) 2-[N-(lS)(2-methyl-l-methoxycarbonylpropyl)carbamoyl]-3-[(2R or S,3S)- 2-hydroxy-3-[N-(2-pyridyl)methoxy-L-valyl]amino-4-phenylbutyl]-2,3- diazabicyclo[2.2. l]heptane, (xvii) 2-t-butoxycarbonyl-3-[(2R or S,3S)-2-hydroxy-3-(N-quinaldoyl-L- asparaginyl)amino-4-phenylbuty 1] -2 , 3-diazabicyclo [2.2.1 ]heptane , (xviii) l-[2-(2-pyridyl)methoxycarbonylamino-]benzoyl-2-[(2R or S,3S)-2- hydroxy-3-(N-quinaldoyl-L-asparaginyl)amino-4-phenylbutyl]-2-isopropyl- hy drazine, (xix) 2-t-butoxycarbonyl-3-[(2R or S,3S)-2-hydroxy-3-(N-quinaldoyl-L- asparaginyl)amino-4-phenylbutyl]-l ,2,3 ,4-tetrahydrophthalazine, (xx) l-trimethylacetyl-2-[(2R or S,3S)-2-hydroxy-3-(phenylmethoxycarbonyl)- amino-4-phyenylbutyl]-2-isopropylhydrazine, (xxi) l-trimethylacetyl-2-[(2R or S,3S)-2-hydroxy-3-(N-quinaldoyl-L- asparaginyl) amino-4-phenylbutyl]-2-isopropylhydrazine, (xxii) l-(t-butylamino)carbonyl-2-[(2R or S,3S)-2-hydroxy-3-(N-quinaldoyl-L- asparaginyl)amino-4-pheny lbutyl] -2-isopropy lhy drazine , (xxiii) t-butyl 3-isopropyl-3-[(2R or S,3S)-2-hydroxy-3-(N-picolinoyl-L- asparaginyl)amino-4-pheny lbutyl] carbazate , (xxiv) t-butyl 3-isopropyl-3-[(2R or S,3S)-2-hydroxy-3-(N-(2-pyridyl)-methoxy- carbonylanthraniloyl)amino-4-pheny lbutyl] carbazate . (xxv) t-butyl 3-benzyl-3-[(2R or S,3S)-2-hydroxy-3-(phenylmethoxycarbonyl)- amino-4-phenylbutyl]carbazate , (xxvi) t-butyl 3-benzyl-3-[(2R or S,3S)-2-hydroxy-3-(N-quinaldoyl-L-asparaginyl)- amino-4-pheny lbutyl] carbazate , (xxvii) t-butyl 3-cyclohexyl-3-[(2R or S, 3S)-2-hydroxy-3-(phenyl-methoxy- carbony l)amino-4-pheny lbutyl] carbazate , (xxviii) t-butyl 3-cyclohexyl-3-[(2R or S,3S)-2-hydroxy-3-(N-quinaldoyl-L- asparaginy l)amino-4-pheny lbutyl] carbazate , (xxix) t-butyl 3-isopropyl-3-[(2R or S,3S)-2-hydroxy-3-(N-(l-carbamoyl-methyl)- acryloyl)amino-4-phenylbutyl]carbazate, (xxx) t-butyl 3-isopropyl-3-[(2R or S,3S)-2-hydroxy-3-(N-(2(RS)-3-tert-butylthio- 2-carbamoyl-methylpropionyl)amino-4-phenylbutyl]carbazate, (xxxi) t-butyl 3-isopropyl-3-[(2R or S,3S)-2-hydroxy-3-(N-(l-benzoyl-L- asparaginyl)amino-4-pheny lbutyl] carbazate , (xxxii) l-t-butyloxycarbonyl-2-[(2R or S,3S)-2-hydroxy-3-(phenylmethoxy- carbony l)amino-4-pheny lbutyl] hexahydropy r idazine , (xxxiii) l-t-butyloxycarbonyl-2-[(2R or S,3S)-2-hydroxy-3-(N-quinaldoyl-L- asparaginy l)amino-4-pheny lbutyl] hexahydropy ridazine , and (xxxiv) cis-1, 6-3-t-butoxycarbonyl-4-[(2R or S, 3S)-2-hydroxy-3-(N-quinaldoyl-3- cyano-L-alanyl)amino-4-phenylbutyl]-3 ,4-diaza-bicyclo [4 ,4,0] decane , wherein the 2-hydroxy group has been derivatised with a solubilising group Px as herein defined. 10. A compound acording to claim 9, wherein said solubilising group is selected from O O II II ^P-OH ^P-OH 0H and H . 5 11. A compound according to claim 10, which compound is selected from the group consisting of: cis-1 , 6-3-t-Butoxycarbony 1-4- [(2S , 3 S)-2-phosphonooxy-3 -(N-quinaldoy 1-L- asparaginyl)amino-4-pheny lbutyl] -3 ,4-diaza-bicyclo [4.4.0] decane ; cis-l,6-3-t-Butoxycarbonyl-4-[(2S, 3S)-2-phosphitooxy-3-(N-quinaldoyl-L- 10 asparaginyl)amino-4-phenylbutyl]-3,4-diaza-bicyclo[4.4.0]decane; t-Butyl 3-isopropyl-3-[(2S, 3S)-2-phosphonooxy-3-(N-quinaldoyl-L-asparaginyl)- amino-4-phenylbutylcarbazate and t-Butyl 3-isopropyl-3-[(2S, 3S)-2-phosphitooxy-3-(N-quinaldoyl-L- asparaginyl)amino-4-phenylbutylcarbazate. 15 12. A process for preparing a compound of formula (I) according to claim 1, said process being selected from the group consisting of: (a) reacting a compound W-(A) n -B-(A*) m -G with a compound H-V; (b) reacting a compound W-(A) n -B-(A*) m -H with a compound G-V; (c) reacting a compound W-H with a compound G-(A) n -B-(A*) m -V; and 0 (d) reacting a compound W-G with a compound H-(A) n -B-(A*) m -V; wherein G is a leaving group; optionally in the presence of a strong base and/or a coupling agent. 13. A process for preparing a compound of formula (IB) according to claim 3 wherein B is a substimted carbon atom and y is 0, said process being selected from: 5 (a) wherein x is 1, reacting a compound of formula (II A), (IIB) or (IIC) with a compound of formula (III) and (b) wherein x is 0, reacting a compound of formula (IIC) or (ED) (IIC) (IID) with a compound of formula (IH) as previously defmed. 14. A process for enhancing the water-solubility of a pharmaceutical or veterinary substance, comprising derivatising a functional group of said substance with a solubilising group Px, wherein Px is selected from the group consisting of Px*, wherein D is O or S, R is H or C r C 4 alkyl, and wherein Px* is selected from: X = O, S, S(O), S(O) 2 said functional group being capable of being derivatised with said solubilising group Px. 15. A process according to claim 14 wherein said substance is an HIV protease 5 inhibitor. 16. A process according to claim 14 wherein said solubilising group Px is selected from O O II II .P-OH and / P"OH OH H 17. A process according to claim 14 comprising reacting a hydroxyl group of said substance with phosphorous acid and optionally oxidising the product so obtained. 10 18. The product of the process of claim 12. 19. The product of the process of claim 14. 20. A pharmaceutical composition comprising an effective amount of a compound of any one of claims 1 to 11, 18 or 19 together with at least one pharmaceutically acceptable carrier, diluent, excipient and/or adjuvant. 15 21. A process for preparing a pharmaceutical composition according to claim 20, comprising mixing a compound according to any one of claims 1 to 11, 18 or 19 with at least one pharmaceutically acceptable carrier, diluent, excipient and/or adjuvant. 22. A method for the treatment or prophylaxis of a retroviral infection, comprising administering to a patient in need of such treatment or prophylaxis a therapeutically 20 effective amount of a compound according to any one of claims 1 to 11, 18 or 19, or of a composition according to claim 20. 23. A method according to claim 22 wherein said retroviral infection is AIDS.

Inventors: GROBELNY DAMIAN, GROBELNY, DAMIAN
Applicants: GROBELNY DAMIAN, NARHEX AUSTRALIA PTY LTD, GROBELNY, DAMIAN, NARHEX AUSTRALIA PTY. LTD.
Application year: 1994
Main classification: C07D255
IPC codes: A61K38, C07C243, C07C251, C07C255, C07C271, C07C281, C07D207, C07D209, C07D211, C07D213, C07D215, C07D231, C07D237, C07D239, C07D243, C07D245, C07D255, C07D257, C07D265, C07D295, C07D303, C07D307, C07D401, C07D403, C07D405, C07D471, C07D487, C07D491, C07D495, C07D498, C07D521, C07F9, C07K5